Annual reports in medicinal chemistry

著者

• Cain, Cornelius K.
• Doherty, Annette M.
• Wood, Anthony
• Macor, John E.
• Desai, Manoj C.
• Neidle, Stephen
• Botta, Maurizio
• American Chemical Society. Division of Medicinal Chemistry

書誌事項

Annual reports in medicinal chemistry

sponsored by the Division of Medicinal Chemistry of the American Chemical Society ; editor-in-chief: Cornelius K. Cain

Academic, 1965-

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注記

Include reference and inxex

v.34-: editor-in-chief: Annette M. Doherty

v.41: editor-in-chief: Anthony Wood

v.42-: editor-in-chief: John E. Macor

v.47-: editor-in-chief: Manoj C. Desai

v.50, 52, 53: editor-in-chief: Stephen Neidle

v.51: editor-in-chief: Maurizio Botta

内容説明・目次

巻冊次

v. 21 ISBN 9780120405213

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

巻冊次

v. 25 ISBN 9780120405251

内容説明

This volume marks the 25th anniversary of issues of "Annual Reports in Medicinal Chemistry". A continuing objective of this series has been to combine regular updates of significant areas of research in medicinal chemistry with emerging areas of biological science destined to make an impact on the future discovery and development of new medicinal agents. Volume 25 retains the familiar format of previous volumes, this year with 35 chapters. Sections I-IV are related to specific medicinal agents, with annual updates on antipsychotics, antihypertensives, antiallergy agents, and antibacterials. Sections V and VI emphasize important emerging areas of medicinal chemistry and biology as well as the interface between these disciplines. Chapters in Section VI reflect the current focus on mechanism-directed drug discovery and newer technologies including PET, catalytic antibodies, and the interface between molecular biology and medicinal chemistry. Trends and perspectives (Section VII) is expanded from previous volumes with chapters on NCE introductions, stereochemistry and drug development, and concludes with a special chapter which provides a perspective on how 25 volumes of "Annual Reports in Medicinal Chemistry" have reflected the evolution of the field of medicinal chemistry over that same time period.

目次

• CNS agents, J.M.McCall
• cardiovascular and pulmonary agents, D.W.Robertson
• chemotherapeutic agents, J.J.Plattner
• metabolic diseases and endocrine function, W.F.Johns
• topics in biology, K.B.Seamon
• topics in chemistry and drug design, F.J.Vinick
• trends and perspectives, J.A. Bristol.

巻冊次

v. 26 ISBN 9780120405268

内容説明

Providing an annual review of advances in the field of medicinal chemistry, and the chemistry of drug development, this book is aimed at pharmacologists, chemists and physicians.

目次

• CNS agents, J.M. McCall
• new anxiolytics, L.J. Browne and K.J. Shaw
• recent advances in excitatory amino acid research, G.Johnson and C.F. Bigge
• progress in anti-depressant drugs, D.W. Robertson and R.W. Fuller
• diversity of neuronal calcium channels, N.A. Saccomano and A.H. Ganong
• recent advances in neurokinin receptor anatagonists, M.E. Logan, et al
• antipsychotics, L.D. Wise and T.G. Heffner
• cardiovascular and pulmonary agents, D.W. Robertson
• angiotensin/renin modulators, W.J. Greenlee and P.K.S. Siegl
• potassium channel activators, J.M. Evans and S.D. Longman
• endogenous vasoactive peptides, A.M. Doherty
• emerging drug discovery targets in thrombosis and coagulation, R.J. Shebuski
• serotonin modulators and cardiovascular/gastrointestinal disease, J.E. Audia and M.L. Cohen
• pulmonary and anti-allergy agents, D.J. Wolanin and J.B. Campbell
• chemotherapeutic agents, J.J. Plattner
• antibacterial agents, K.E. Brighty and P.R. McGuirk
• antiviral agents, M.M. Mansuri and J.C. Martin
• HIV protease inhibitors, D.W. Norbeck and D.J. Kempf
• radiosensitizers, M.J. Suto
• antiparasitic agents, D.M. Schmatz and J.M. Schaeffer
• function of human retrovirus regulatory proteins, C.A. Rosen and S.M. Ruben
• immunology, endocrinology and metabolic diseases, W.F. Michne
• chemical basis for immune mediated idiosyncratic drug hypersensitivity, M.A. Sanner and T.J. Higgins
• cholecystokinin agonists and antagonists, A.M. Nadzan and J.F. Kerwin
• recent advances in bone metabolism and osteoporosis research, T.J. Caggiano, et al
• mechanism-based immunosuppressants, J.R. Luly
• topics in biology, K.B. Seamon
• cytokin receptors, D.L. Urdal
• amyloidogenesis as a therapeutic target in Alzheimer's disease, B.D. Greenberg and F.J. Kezdy
• bacterial adhesins, J. London
• regulation of the ras GTPase cycle, G. Bollag, et al
• topics in drug design and discovery, M.C. Venuti
• the search for molecular diversity (1) natural products, L.J. Nisbet and P.J. Hylands
• the search for molecular diversity (2) recombinant and synthetic randomized peptide libraries, W.J. Dower and S.P.A. Fodor
• receptor modeling by distance geometry, J.M. Blaney and J.S. Dixon
• sequence-defined oligonucleotides as potential therapeutics, M.D. Matteucci and N. Bischofberger
• trends and perspectives, J.A. Bristol
• to market, to market - 1990, J.D. Strupczewski, et al
• perspectives on human gene therapy, G.J. Nabel and E.G. Nabel.

巻冊次

v. 27 ISBN 9780120405275

内容説明

Intended for medicinal, pharmaceutical and organic chemists, this serial combines regular updates of significant areas of research in medicinal chemistry with emerging areas of biological science destined to affect the future discovery and development of new medicinal agents.

目次

• Part 1 Agents: the decade of the brain, M. Williams
• pharmacological intervention in sleep and circadian processes, J.D. Miller
• advances in central serotoninergics, A.G. Romero and A.B. McCall
• traumatic and ischemia/reperfusion injury to the CNS, J.M. McCall and J.A. Panetta
• trophic factors and their receptors in the CNS, S. Rosenberg
• antipsychotics, L.D. Wise and T.G. Heffner. Part 2 Cardiovascular and pulmonary agents: angiotensin/renin modulators, W.J. Greenlee and P.K.S. Siegl
• EDRF, an emerging target for drug design, J.F. Kerwin, Jr
• endogenous vasoactive peptides, A.M. Doherty
• recent advances in antiarrhythmic therapy - potassium channel antagonists, M.G. Cimini and J.K. Gibson
• future antithrombotic therapy, J.A. Jakubowski, et al
• pulmonary and anti-allergy agents, R.T. Jacobs, et al. Part 3 Chemotherapeutic agents: antibacterial agents, targets, and approaches, M.J. Suto, et al
• genetic engineering of antibiotic producing organisms, L. Katz and C.R. Hutchinson
• inhibitors of angiogenesis, M.A. Mitchell and J.W. Wilks
• recent advances in antifungal agents, J.F. Barrett and D.H. Klaubert
• progress in antimicrobial peptides, S.W. Blondelle and R.A. Houghten
• protein tyrosine kinases and cancer, E.M. Dobrusin and D.W. Fry. Part 4 Immunology, endocrinology, and metabolic diseases: monoclonal antibodies in therapy, G.A. Heavner
• techniques for determining epitopes for antibodies and T-cell receptors, D.C. Benjamin and S.S. Perdue
• potential therapeutic modifiers of the complement cascade, W.K. Hagmann and R.D. Sindelar
• cytokine modulation as medicinal chemistry target, K. Cooper and H. Masamune
• recent advances in the discovery and development of potential antidiabetic agents, J.R. Colca and S.P. Tanis. Part 5 Topics in biology: the role of homeobox genes in vertebrate embryonic development, K. Mahon and M. Jamrich
• emerging therapies for cystic fibrosis, A.E. Smith
• the guanylyl cyclase family of receptor/enzymes, H.-J. Fulle and D.L. Garbers
• HIV vaccine development - from empiricism to medicinal chemistry, M.J. Glass and W.C. Kogg
• inositol triphosphate receptors, S.K. Joseph. Part 6 Topics in drug design and discovery: macromolecular X-ray crystalloglraphy and NMR as tools for structure-based drug design, J.W. Erickson and S.W Fesik. Part contents.

巻冊次

v. 28 ISBN 9780120405282

内容説明

This serial combines regular updates of significant areas of research in medicinal chemistry with emerging areas of biological science destined to impact the future discovery and development of new medicinal agents. Topics in this volume include CNS agents and chemotherapeutic agents.

目次

J.M. McCall, CNS Agents. D.W. Robertson, Cardiovascular and Pulmonary Agents. J.J. Plattner, Chemotherapeutic Agents. W.K. Hagmann, Immunology, Endocrinology and Metabolic Diseases. K.B. Seamon, Topics in Biology. M.C. Venuti, Topics in Drug Design and Discovery. J.A. Bristol, Trends and Perspectives.

巻冊次

v. 29 ISBN 9780120405299

内容説明

This serial continues to combine regular updates of significant areas of research in medicinal chemistry with emerging areas of biological science destined to impact the discovery and development of new medicinal agents.

目次

• Part 1 CNS agents: third generation antidepressants
• neuronal cell death
• muscarinic agonists and antagonists
• animal engineering in neurobiology
• dopamine D3 and D4 receptor ligands and pharmacology
• excitatory amino acid research. Part 2 Cardiovascular and pulmonary agents: endothelin receptor antagonists
• treatment of asthma and allergy
• nitric oxide synthase
• thrombolytic agents
• antithrombotic and anti-inflammatory agents. Part 3 Chemotherapeutic agents: antibacterial agents
• HIV reverse transcriptase inhibitors
• HIV protease inhibitors
• ras oncogene. Part 4 Immunology, endocrinology and metabolic diseases: non-immunophilin-related immunosuppressants
• phosphodiesterase inhibitors as antiasthmatic agents
• human leukocyte elastase inhibitors
• interleukin-1
• cell adhesion and carbohydrates
• control of androgen action. Part 5 Topics in biology: transcription factor NF-kB
• translational control of gene expression
• protein kinases and photophatases
• transgenic and gene targeting technology
• osteoporosis. Part 6 Topics in drug design and discovery: adenylate cyclase subtypes
• advances in antisense technology
• prediction of human drug metabolism
• humanized monoclonal antibodies
• ethnobotany. Part 7 Trends and perspectives: to market, to market - 1993
• appendices.

巻冊次

v. 30 ISBN 9780120405305

内容説明

Praise for the Series: This series is one of the very few annual publications which justify the title of an absolute must for the pharmacologist, chemist, or physician who is interested in the chemistry of drug development. --Enzymologia This book is strongly recommended for researchers, teachers, students, administrators - in short, anyone whose interests impinge on medicinal chemistry. In view of the work's documented reference value, it is a must for inlusion in the scientist's personal library. --Journal of Medicinal Chemistry All topics are covered in sufficient depth, with extensive references, to allow either the specialist or the novice to be informed of the latest developments in a particular area of medicinal chemistry. --Norman Gilman, Hoffmann-La Roche, Inc, in the JOURNAL OF PHARMACEUTICAL SCIENCES Advances in Medicinal Chemistry continues to provide timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

• Central nervous system diseases
• cardiovascular and pulmonary diseases
• cancer and infectious diseases
• immunology, endocrinology and metabolic diseases
• topics in biology
• topics in drug design and discovery
• trends and perspectives.

巻冊次

v. 31 ISBN 9780120405312

内容説明

Advances in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

• Central nervous system diseases
• cardiovascular and pulmonary diseases
• cancer and infectious diseases
• immunology, endocrinology and metabolic diseases
• topics in biology
• topics in drug design and discovery
• trends and perspectives.

巻冊次

v. 32 ISBN 9780120405329

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expectedto provide the basis for entirely new future therapies.

目次

• Part 1 Central nervous system diseases, D.W. Robertson: recent advances in migraine therapy, T. Branchek and J.E. Audia
• Alzheimer's disease - recent advances on the amyloid hypothesis, V. John et al
• obesity - leptin-neuropeptide Y interactions in the control of body weight, D.R. Gehlert and M. Heiman
• melatonin receptor ligands and their potential clinical applications, C.D. Mahle et al
• corticotrophin-releasing hormone (CRH) receptors and the discovery of selective non-peptide CRH1 antagonists, P.J. Gilligan et al
• recent advances in neurokinin receptor antagonists, S.G. Mills. Part 2 Cardiovascular and pulmonary diseases, A.M. Doherty: endothelin inhibitors, X.-M. Cheng et al
• antithrombotics/serine proteases, W.C. Ripka and G.P. Vlasuk
• leukotriene modulators as therapeutic agents in asthma and other inflammatory diseases, R.L. Bell et al
• emerging opportunities in the treatment of atherosclerosis, C.M. Hayward and M.J. Bamberger. Part 3 Cancer and infectious diseases, J.J. Plattner: new approaches and agents to overcome bacterial resistance, J.M. Domagala and J.P. Sanchez
• bacterial genomics and the search for novel antibiotics, L. Katz et al
• resistance to antiretroviral drug therapy, A. Molla and W.E. Kohlbrenner
• non-HIV antiviral agents, S.H. Krawczyk and N. Bischofberger
• recent advances in antifungal agents, P.A. Lartey and C.M. Moehle
• angiogenesis inhibitors, D. Powell et al
• chemical inhibitors of cyclin-dependent kinases, K.G. Coleman et al. Part 4 Immunology, endocrinology and metabolic diseases, W.K. Hagmann: T lymphocyte potassium channel blockers, J.C. Kath et al
• male contraception, D.W. Combs
• new dermatological agents for the treatment of psoriasis, S. Nagpal and R.A.S. Chandraratna
• selective cyclooxygenase-2 inhibitors, P. Prasit and D. Riendeau
• growth hormone secretagogues, R.P. Nargund and L.H.T. Van der Ploeg. Part 5 Topics in biology, W.W. Wong: novel gene switches for the regulation of gene expression
• agents that block TNF-I synthesis or activity, R.A. Black et al
• nuclear orphan receptors - scientific progress and therapeutic opportunities, D.W. Robertson et al. Part 6 Topics in drug design and discovery, G.L. Trainor: discovery and identification of lead compounds from combinational mixtures, B.A. Beutal
• electrospray mass spectrometric characterization of adducts between therapeutic agents and proteins, C. Fenselau
• nonpeptide agonists for peptide receptors - lessons from ligands, E.E. Sugg
• natural products research and pharmaceuticals in the 1990s, S.K. Wrigley and M.I. Chicarelli-Robinson
• inhibition of cytochrome P-450 and implications in drug development, J.H. Lin and A.Y.H. Lu. Part 7 Trends and perspectives, J.A. Bristol: to market, to market - 1996, P. Galatsis.

巻冊次

v. 33 ISBN 9780120405336

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expectedto provide the basis for entirely new future therapies.

目次

I. Central Nervous System Agents II. Cardiovascular and Pulmonary Diseases III. Cancer and Infectious Diseases IV. Immunology, Endocrinology and Metabolic Diseases V. Topics in Biology VI. Topics in Drug Design and Discovery VII. Trends and Perspectives

巻冊次

v. 34 ISBN 9780120405343

内容説明

Annual Reports in Medicinal Chemistry continues to strive to provide timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences which are expected to provide the basis for entirely new future therapies. Volume 34 retains the familiar format of previous volumes, this year with 33 chapters. Sections I-IV are disease-oriented and generally report on specific medicinal agents with updates from Volume 33 on antithrombotics, neurokinin receptor antagonists, anticoagualants, and new antibacterials. As in past volumes, annual updates have been limited to only the most active areas of research in favor of specifically focused and mechanistically oriented chapters, where the objective is to provide the reader with the most important new results in a particular field. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design as well as the critical interfaces among these disciplines. This volume concludes with To Market, To Market--a chapter on NCE and NBE introductions worldwide in 1998, a chapter on pharmagenomics, and finally one on malaria as a third world disease in need of a first world drug development.

目次

• Section Editor: D.W. Robertson, Central Nervous System Diseases. Section Editor: W.J. Greenlee, Cardiovascular and Pulmonary Diseases. Section Editor: J.J. Plattner, Cancer and Infectious Diseases. Section Editor: W.K. Hagmann, Immunology, Endocrinology, and Metabolic Diseases. Section Editor: W.W. Wong, Topics in Biology. G.L. Trainor, Topics in Drug Design and Discovery. Section Editor: A.M. Doherty, Trends and Perspectives.
• D.A. Evrard and B.L. Harrison, Recent Approaches to Novel Antidepressant Therapy. J.R. McCarthy, S.C. Heinrichs, and D.E. Grigoriadis, Recent Progress in Corticotropin-Releasing Factor Receptor Agents. C.E. Augelli-Szafran, L.C. Walker, and H. LeVine III, -Amyloid as a Target for Alzheimer's Disease Therapy. A.W Stamford and E.M. Parker, Recent Advances in the Development of Neuropeptide Y Receptor Antagonists. K.S. Takaki and J.R. Epperson, Pharmacological Interventions in the Sleep Process. C. Swain and N.M.J. Rupniak, Progress in the Development of Neurokinin Antagonists.

巻冊次

v. 35 ISBN 9780120405350

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences which are expected to provide the basis for entirely new future therapies.

巻冊次

v. 36 ISBN 9780120405367

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

巻冊次

v. 37 ISBN 9780120405374

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

I. CENTRAL NERVOUS SYSTEM DISEASES Section Editor: David W. Robertson, Pfizer Global Research & Development, Ann Arbor, MI II. CARDIOVASCULAR AND PULMONARY DISEASES Section Editor: William J. Greenlee, Schering-Plough Research Institute, Kenilworth, New Jersey III. CANCER AND INFECTIOUS DISEASES Section Editor: Jacob J. Plattner, Chiron Corporation, Emeryville, California IV. IMMUNOLOGY, ENDOCRINOLOGY AND METABOLIC DISEASES Section Editor: William K. Hagmann, Merck Research Laboratories, Rahway, New Jersey V. TOPICS IN BIOLOGY Section Editor: Janet M. Allen, Inpharmatica, London, United Kingdom VI. TOPICS IN DRUG DESIGN AND DISCOVERY Section Editor: George L. Trainor, DuPont Pharmaceuticals Company, Wilmington, Delaware VII. TRENDS AND PERSPECTIVES Section Editor: Annette M. Doherty, Pfizer Global Research & Development, Fresnes Laboratories, Fresnes, France

巻冊次

v. 38 ISBN 9780120405381

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

CENTRAL NERVOUS SYSTEM DISEASES. CARDIOVASCULAR AND METABOLIC DISEASES. INFLAMMATORY, PULMONARY, AND GASTROINTESTINAL DISEASES. CANCER AND INFECTIOUS DISEASES. TOPICS IN BIOLOGY. TOPICS IN DRUG DESIGN AND DISCOVERY. TRENDS AND PERSPECTIVES.

巻冊次

v. 39 ISBN 9780120405398

内容説明

Annual Reports in Medicinal Chemistry continues to focus on providing timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design.

目次

I. CENTRAL NERVOUS SYSTEM DISEASES. II. CARDIOVASCULAR AND METABOLIC DISEASES. III. INFLAMMATORY, PULMONARY, AND GASTROINTESTINAL DISEASES. IV. CANCER AND INFECTIOUS DISEASES. V. TOPICS IN BIOLOGY. VI. TOPICS IN DRUG DESIGN AND DISCOVERY. VII. TRENDS AND PERSPECTIVES.

巻冊次

v. 40 ISBN 9780120405404

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design. Section VII looks at Trends and Perspectives in the pharmaceuticals market.

目次

I. Central Nervous System Diseases II. Cardiovascular and Metabolic Diseases III. Inflammatory, Pulmonary, and Gastrointestinal Diseases IV. Cancer and Infectious Diseases V. Topics in Biology VI. Topics in Drug Design and Discovery VII. Trends and Perspectives

巻冊次

v. 41 ISBN 9780120405411

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design. Section VII looks at Trends and Perspectives in the pharmaceuticals market.

目次

I. Central Nervous System Diseases (A.J. Robichaud). II. Cardiovascular and Metabolic Diseases (A. Stamford). III. Inflammatory, Pulmonary, and Gastrointestinal Diseases (M.G. Bock). IV. Cancer and Infectious Diseases (D. Myles). V. Topics in Biology (D. Cohen). VI. Topics in Drug Design and Discovery (M.C. Desai). VII. Trends and Perspectives (A. Wood).

巻冊次

v. 42 ISBN 9780123739124

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

Central Nervous System Diseases Cardiovascular and Metabolic Diseases Inflammation, Pulmonary and Gastro Intestinal Diseases Cancer and Infectious Diseases Topics in Biology Topics in Drug Design and Discovery To Market, To Market 2006 Indexes including cumulative NCE indexes

巻冊次

v. 43 ISBN 9780123743442

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

• Part I. Central Nervous System Diseases C ROBICHAUD Chapter 1 Recent Advances in Corticotropin Releasing Factor Receptor Antagonists Carolyn D. Dzierba
• Richard A. Hartz
• Joanne J. Bronson Chapter 2 Recent Advances on the 5-HT5A, 5-HT6 and 5-HT7 Receptors Brock T. Shireman, Pascal Bonaventure and Nicholas I. Carruthers Chapter 3 Recent Advances in Voltage Gated Sodium Channel Blockers: Therapeutic Potential as Drug Targets in the CNS Andreas Termin, Esther Martinborough and Dean Wilson Chapter 4 Medication Development for the Treatment of Substance Abuse Brian Fulton Part II. Cardiovascular and Metabolic Diseases - STAMFORD Chapter 5 GPR40 (FFAR1) Modulators Julio C. Medina and Jonathan B. Houze Chapter 6 Rho-Kinase Inhibitors for Cardiovascular Disease Robert A. Stavenger Chapter 7 LXR Agonists for the Treatment of Atherosclerosis - Recent Highlights Jonathan Bennett, Andrew Cooke, Heather J. McKinnon and Olaf Nimz Chapter 8 Glucagon Receptor Antagonists for Type II Diabetes DuaneE. DeMong, Michael W. Miller and Jean Lachowicz Part III. Inflammation / Pulmonary / GI C BARRISH Chapter 9 Advances Towards Dissociated Non-Steroidal Glucocorticoid Receptor Agonists John Regan, Hossein Razavi, David Thomson Chapter 10 Advances in the Discovery of IkB Kinase Inhibitors William J. Pitts and James Kempson Chapter 11 Protease Inhibitors for the Potential Treatment of Chronic Obstructive Pulmonary Disease and Asthma Weimin Liu and Eugene Hickey Part IV. Oncology - MYLES Chapter 12 mTor Inhibitors in Oncology Jeroen Verheijen, Ker Yu and Arie Zask Chapter 13 Oncology Drug Targets in the Sphingomyelin Signaling Path Bill Garland, Amy Cavalli and Genevive Hansen Part V. Infectious Diseases - Primeau Chapter 14 Inhibitors of Respiratory Syncytial Virus Malcolm Carter and G. Stuart Cockerill Chapter 15 Recent Developments in |A-Lactamases and Inhibitors Tarek S. Mansour, Patricia A. Bradford and Aranapakam M. Venkatesan Chapter 16 Recent Development in the Treatment of Clostridium Difficile Associated Disease (CDAD) Xicheng Sun, Joseph Guiles and Nebojsa Janjic Chapter 17 Recent Advances in the Discovery of Hybrid Antibacterial Agents Mike Barbachyn Part VI. Topics in Biology - LOWE Chapter 18 Recent Renaissance of Prostaglandin Research Robert Burk Chapter 19 Human Exposure and Dose Projections Punit H. Marathe, Christine Huang and A. David Rodrigues Chapter 20 Modeling Networks of Glycolysis, Overall Energy Metabolism and Drug Metabolism under a Systems Biology Approach Zoltan Sarnyai and Laszlo G. Boros Part VII. Topics in Drug Design and Discovery C DESAI Chapter 21 Contrasting the Gastrointestinal Tracts of Mammals: Factors that Influence Absorption John DeSesso and Amy Lavin Williams Chapter 22 The Emerging Utility of Co-Crystals in Drug Discovery and Development Nicholas Meanwell Chapter 23 Pregnane X Receptor: Prediction and Attenuation of Human CYP3A4 Enzyme Induction and Drug-Drug Interactions Michael W. Sinz Chapter 24 Formulation in Drug Discovery Robert Strictly Part VIII. To Market, To Market Chapter 25 To Market, To Market - 2007 Shridhar Hegde and Michelle Schmidt

巻冊次

v. 44 ISBN 9780123747662

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

1 Recent advances in the discovery of GSK-3 inhibitors and a perspective on their utility for the treatment of Alzheimer's disease Robert G. Gentles, Shuanghua Hu, and. Gene Dubowchik 2 Advances in the Development of Nitric Oxide Synthase Inhibitors Shawn Maddaford, Subhash Annendi, Jailall Remnauth, and Suman Rakhit 3 Small Molecule Protein-Protein Interaction Inhibitors as Therapeutic Agents for Neurodegenerative Diseases: Current Progress and Future Hurdles Simon Haydar and Warren Hirst 4 Case History: Chantix (varenicline tartrate) a Nicotinic Partial Agonist Aid to Smoking Cessation Jotham W. Coe, Hans Rollema and Brian T. O'Neill 5 Case History on Tekturna (R) /Rasilez (R) (Aliskiren), a Highly Efficacious Direct Oral Renin Inhibitor as a New Therapy for Hypertension Juergen Maibaum and David Feldman 6 Advances in Vasopressin Receptor Agonists and Antagonists Thomas Ryckmans 7 The Emergence of GPR119 Agonists as Anti-diabetic Agents Robert Jones 8 Non-peptide Ligands for the Gonadotropin Receptors Nicole van Straten, Marco Timmers 9 Recent Advances in Coagulation Serine Protease Inhibitors Mimi Quan and Joanne Smallheer 10 Advances in the Discovery of Anti-Inflammatory FMS Inhibitors Mark Player and Carl Manthey 11 Recent Advances in the Discovery of CB2 Selective Agonists Jayant Thatte, Sangdon Han, and Rob Jones 12 Advances in the Discovery of Small Molecule JAK3 Inhibitors Stephen Wrobleski 13 Recent Advances in Adenosine Receptor (AR) Ligands in Pulmonary Diseases Jeff Zablocki and Rao Kalla 14 Recent Progress in the Development of Small Molecule Inhibitors of Insulin-like Growth Factor Receptor (IGF-1R) Kinase Dinesh Vyas and Mark Wittman 15 Case History: Discovery of Ixabepilone (IXEMPRA[TM]), a First-inclass Epothilone Analogue for Treatment of Metastatic Breast Cancer Robert M. Borzilleri and Gregory D. 16 Hedgehog Signaling Pathway Inhibitors as Cancer Therapeutics Stefan Peuker and Karen Miller-Moslin 17 Emerging Therapies Based on Inhibitors of Phosphatidyl-Inositol- 3-Kinases (PI3Ks) John M. Nuss, Amy Lew Tsuhako and Neel K. Anand Exelixis 18 Anti-infective Activity of Artemisinin and its Semi-synthetic Derivatives John G. D'Angelo 19 Recent Advances in the Inhibition of Bacterial Type II Topoisomerases Greg Bisacchi & Jacques Dumas 20 Progress Towards the Discovery and Development of Specifically Targeted Inhibitors of Hepatitis C Virus Nicholas A. Meanwell John F. Kadow and Paul M. Scol 21 Inhibitors of Nuclear Hormone Receptor/Steroid Receptor Coactivator Interactions Terry Moore, John Katzenellenbogen 22 Safety Testing of Drug Metabolites Tom Thompson 23 A Path to Innovation: Gene Knockouts Model New Drug Action Brian Zambrowicz 24 Discovery of Novel Positron Emission Tomography (PET) Tracers Dennis McCarthy 25 The Use of Isotopically Labeled Compounds in Drug Discovery (Chad) Charles S. Elmore 26 Mechanism based inhibition of CYP3A4 and other cytochromes P450 Bernard Murray 27 Nonclinical Toxicogenomics in the Pharmaceutical Environment Bruce D. Car 28 To Market, To Market 2008 Shridhar Hegde and Michelle Schmidt

巻冊次

v. 45 ISBN 9780123809025

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

Section I: Central Nervous System Diseases - ROBICHAUD Voltage-Gated Calcium Channel Antagonists for the Central Nervous System James C. Barrow and Joseph L. Duffy Recent Developments in Glycine Transporter-1 Inhibitors Christopher L. Cioffi, Shuang Liu and Mark A.Wolf Modulators of Transient Receptor Potential Ion Channels Rajagopal Bakthavatchalam and S. David Kimball Defining Neuropharmacokinetic Parameters in CNS Drug Discovery to Determine Cross-species Pharmacologic Exposure-Response Relationships Christopher L. Shaffer Section II: Cardiovascular and Metabolic Diseases - STAMFORD High Affinity Niacin Receptor GPR109A Agonists Hong C. Shen and Steven L. Colletti Recent Advances in Acetyl CoA Carboxylase (ACC) Inhibitors Matthew P. Bourbeau, John G. Allen, and Wei Gu Enzymatic Targets in the Triglyceride Synthesis Pathway Dmitry O. Koltun and Jeff Zablocki Inhibitors of HIF Prolyl Hydroxylases Michael H. Rabinowitz, Terrance D. Barrett, Mark D. Rosen, Hariharan Venkatesan Section III: Inflammation / Pulmonary / GI - BARRISH/Weinstein Opioid Receptor Antagonists for Gastrointestinal Dysfunction R. William Hipkin and Roland E. Dolle CFTR Modulators for the Treatment of Cystic Fibrosis Sabine Hadida, Frederick Van Goor and Peter D. J. Grootenhuis Targeting B-cells in inflammatory disease Kevin S. Currie Modulators of Toll-Like Receptor (TLR) Signaling Mark Spyvee, Lynn Hawkins, and Sally Ishizaka Section IV: Oncology - McAlpine Janus Kinase 2 (JAK2) inhibitors for the treatment of myeloproliferative neoplasm (MPN) Ashok V. Purandare, Matthew V. Lorenzi and Louis J. Lombardo Development of poly(ADP-ribose)polymerase (PARP) inhibitors in oncology Philip Jones Epigenetic Targets and Cancer Drug Discovery Patrick M. Woster, Ph.D Section V: Infectious Diseases - Primeau HIV-1 Integrase Strand Transfer Inhibitors Brian A. Johns Recent Advances in Drug Discovery for Neglected Tropical Diseases Caused by Infective Kinetoplastid Parasites Robert T. Jacobs and Charles Ding Recent Advances in the Inhibition of Bacterial Fatty Acid Biosynthesis Vincent Gerusz Section VI: Topics in Biology - LOWE Back to the Plaque: Emerging Studies That Re-Focus Attention on the Neuritic Plaque in Alzheimer's Disease Dr. Robert B. Nelson Targeting Methyl Lysine Stephen V. Frye, Tom Heightman and Jian Jin Chemical Proteomic Technologies for Drug Target Identification Kieran F. Geoghegan and Douglas S. Johnson NIH Translational Programs for Assisting Pre-Clinical Drug Discovery and Development Raj N. Misra Section VII: Topics in Drug Design and Discovery - DESAI Role of Physicochemical Properties and Lipophilic Ligand Efficiency (LipE or LLE) in addressing Drug Safety Risks Martin P. Edwards and David A. Price Reducing the Risk of Drug Attrition Associated with Physicochemical Properties Paul D. Leeson and James R. Empfield Compound Collection Enhancement and Paradigms for High Throughput Screening - an Update Stevan W Djuric, Irini Akritopoulou-Zanze, Philip B Cox and Scott Galasinski The Role of Fluorine in the Discovery and Optimization of CNS Agents: Modulation of Drug-Like Properties Kevin J. Hodgetts, Kerry J. Combs, Amy M. Elder and Geraldine C. Harriman Patents in Drug Discovery: Case Studies, Examples, and Simple Steps Medicinal Chemists Can Take to Protect Hard-Won Intellectual Property Charles J. Andres, Jr. and Richard L. Treanor Section VIII: Trends and Perspectives To Market, To Market - 2009 Shridhar Hegde and Michelle Schmidt

巻冊次

v. 46 ISBN 9780123860095

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

1 mGlu4 Modulators Kevin Liu2 Recent Advances towards Pain Therapeutics Philippe Nantermet3 Circadian Rythym Paul Galatsis4 Recent Progress in the Discovery of Kv7.x Modulators' Ismet Dorange5 Bile Acid Receptor Modulators for Treatment of Metabolic Diseases Yanping Xu6 Mineralocorticoid Receptor Antagonists Katerina Leftheris7 SGLT2 Inhibitors for the Treatment of Diabetes Jiwen Liu, TaeWeon Lee8 CRTh2 Antagonists Laurence E. Burgess9 Developments and Advances in Gastrointestinal Prokinetic Agents James W. Dale10 Targeting Th17 and Treg Signaling Pathways in Autoimmunity Shomir Ghosh11 Advances in the Discovery of C5a Receptor Antagonists Jay P. Powers12 Inhibition of Translation Initiation as a Novel Paradigm for Cancer13 The Development of Inhibitor of Apoptosis Protein Antagonists for the Treatment of Resistant Cancers. Stephen Condon14 Case History on the Discovery of Halaven (R) Melvin Lu15 Emerging New Therapeutics against Key Gram-negative Pathogens Daniel Obrecht16 Hepatitis C Virus Inhibitors - Beyond NS3 Protease and NS5B17 The Emergence of Small Molecule Modulators of the Capsid Assembly Pathway as Potential Antiviral Therapeutics Clarence R. Hurt 18 Mechanism of Action (MoA) in Drug Discovery David Swinney19 Aryl Hydrocarbon Receptor (AhR) Activation: An Emerging20 Prolyl Isomerases Pat Flaherty21 Potential Therapeutic Applications of miRNA Graham Brock22 Induced Pluripotent Stem Cells (iPSC) as Drug Discovery Tools and Human Disease Models Charles R. Johnson23 Progress in Drug Repositioning: Old Drugs, New Opportunities Michael A. Walters 24 Deuterium in Drug Discovery and Development Scott L. Harbeson25 Phospholipidosis Peter Bernstein26 To Market, To Market 2010 Joanne Bronson

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v. 47 ISBN 9780123964922

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

• Personal Essay Reflections on Medicinal Chemistry at Merck, West Point Paul S. Anderson My Path in Seeking New Medicines Peter R. Bernstein Tales of Drug Discovery M. Ross Johnson I. Central Nervous System Diseases Section Editor: Albert J. Robichaud
• Sage Therapeutics, Inc. Cambridge, Massachusetts Recent Developments in Targeting Neuroinflammation in Disease Allen T. Hopper, Brian M. Campbell, Henry Kao, Sean A. Pintchovski and Roland G. W. Staal Secretase Inhibitors and Modulators as a Disease Modifying Approach Against Alzheimer's Disease Harrie J. M. Gijsen and Francois P. Bischoff mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders Sylvain Celanire, Guillaume Duvey, Sonia Poli and Jean-Philippe Rocher NMDA Antagonists of GluN2B Subtype and Modulators of GluN2A, GluN2C and GluN2D Subtypes - Recent Results and Developments Kamalesh B. Ruppa, Dalton King and Richard Olson Recent Advances in the Development of PET and SPECT Tracers for Brain Imaging Lei Zhang and Anabella Villalobos II. Cardiovascular and Metabolic Diseases Section Editor: Andy Stamford, Merck Research Laboratories, Kenilworth, New Jersey Case History: EliquisTM (Apixaban), a Potent and Selective Inhibitor of Coagulation Factor Xa for the Prevention and Treatment of Thrombotic Diseases Donald J. P. Pinto, Pancras C. Wong, Robert M. Knabb and Ruth R. R. Wexler AMPK Activation in Health and Disease Iyassu K. Sebhat and Robert W. Myers Type-2 Diabetes and Associated Co-Morbidities as an Inflammatory Syndrome Juan C. Jaen, Jay P. Powers and Tim Sullivan Beyond PPARs & Metformin: New Insulin Sensitizers for the Treatment of Type 2 Diabetes Philip A. Carpino and David Hepworth III. Inflammatory Pulmonary and Gastrointestinal Diseases Section Editor: David S. Weinstein, Bristol-Myers Squibb R&D, Princeton, New Jersey Recent Advances in the Discovery and Development of Sphingosine-1-Phosphate-1 Receptor Agonists Alaric J. Dyckman Bifunctional Compounds for the Treatment of COPD Gary Phillips and Michael Salmon Inflammatory Targets for the Treatment of Atherosclerosis Robert O. Hughes, Alessandra Bartolozzi and Hidenori Takahashi IV. Oncology Section Editor: Shelli R. McAlpine, School of Chemistry, University of New South Wales, Sydney, Australia Nanotechnology Therapeutics in Oncology - Recent Developments and Future Outlook Paul F. Richardson Small-Molecule Antagonists of Bcl-2 Family Proteins Sean P. Brown and Joshua P. Taygerly Notch Pathway Modulators as Anti-Cancer Chemotherapeutics Vibhavari Sail and M. Kyle Hadden Anaplastic Lymphoma Kinase (ALK) Inhibitors for the Treatment of ALK-Positive Cancers Kazutomo Kinoshita, Nobuhiro Oikawa and Takuo Tsukuda V. Infectious Diseases Section Editor: John Primeau, Westford, Massachusetts Recent Advances in the Discovery of Dengue Virus Inhibitors Jeremy Green, Upul Bandarage, Kate Luisi and Rene Rijnbrand Non Fluoro-Quinolone Based Inhibitors of Mycobacterial Type II Topoisomerase as Potential Therapeutic Agents for TB Pravin S. Shirude and Shahul Hameed HCV Inhibition Mediated through the Nonstructural Protein 5A (NS5A) Replication Complex Robert Hamatake, Andrew Maynard and Wieslaw M. Kazmierski VI. Topics in Biology Section Editor: John Lowe, JL3Pharma LLC, Stonington, Connecticut Antibody-Drug Conjugates for Targeted Cancer Therapy Victor S. Goldmacher, Thomas Chittenden, Ravi V. J. Chari, Yelena V. Kovtun and John M. Lambert 3D Cell Cultures: Mimicking in Vivo Tissues for Improved Predictability in Drug Discovery Indira Padmalayam and Mark J. Suto Virally Encoded G Protein-Coupled Receptors: Overlooked Therapeutic Opportunities? Nuska Tschammer Recent Advances in Wnt/b-Catenin Pathway Small Molecule Inhibitors Daniel D. Holsworth and Stefan Krauss VII. Topics in Drug Design and Discovery Section Editor: Peter R. Bernstein, PhaRmaB LLC, Rose Valley, Pennsylvania Targeted Covalent Enzyme Inhibitors Mark C. Noe and Adam M. Gilbert Drug Design Strategies for GPCR Allosteric Modulators P. Jeffrey Conn, Scott D. Kuduk and Dario Doller Progress in the Development of Non-ATP Competitive Protein Kinase Inhibitors for Oncology Campbell McInnes VIII. Trends Section Editor: Joanne Bronson, Bristol-Myers Squibb, Wallingford, Connecticut New Chemical Entities Entering Phase III Trials in 2011 Gregory T. Notte To Market, To Market - 2011Joanne Bronson, Murali Dhar, William Ewing and Nils Lonberg

巻冊次

v. 48 ISBN 9780124171503

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

目次

Challenges in Drug Discovery at Schering-Plough Research Institute: A Personal Reflection My Perspective on Time, Managers-and Scientific Fun A Career in Medicinal Chemistry - A Journey in Drug Discovery Selective Inhibitors of PDE2, PDE9 and PDE10 - Modulators of Activity of the Central Nervous System Beyond Secretases: Kinases Inhibitors for the Treatment of Alzheimer's Disease Orexin Receptor Antagonists in Development for Insomnia and CNS Disorders Discovery and Development of Prolylcarboxypeptidase (PRCP) Inhibitors for Cardiometabolic Disorders Molecular Targeting of Imaging and Drug Delivery Probes in Atherosclerosis Oral GLP-1 Modulators for the Treatment of Diabetes Recent Advances in the Discovery and Development of CCR1 Antagonists Emerging Targets for the Treatment of Idiopathic Pulmonary Fibrosis Targeting the Nuclear Hormone Receptor RORgt for the Treatment of Autoimmune and Inflammatory Disorders Recent Advances in Small-Molecule Modulation of Epigenetic Targets: Discovery and Development of Histone Methyltransferase- and Bromodomain Inhibitors Inhibition of Ubiquitin Proteasome System Enzymes for Anticancer Therapy Targeting Protein-Protein Interactions to Treat Cancer?Recent Progress and Future Directions Recent Progress in the Discovery of Neuraminidase Inhibitors as Anti-influenza Agents Novel Therapeutics in Discovery and Development for Treatment of Chronic HBV Infection Special Challenges to the Rational Design of Antibacterial Agents Recent Advances in Small Molecule Target Identification Methods Neuroinflammation in Mood Disorders: Mechanisms and Drug Targets Inhibitors of hERG Channel Trafficking-A Cryptic Mechanism For QT Prolongation Recent Progress in Small-Molecule Agents Against Age-Related Macular Degeneration Synthetic Macrocycles in Small-Molecule Drug Discovery Glossary of Terms Used in Medicinal Chemistry Part II (IUPAC Recommendations 2011) Case History: XalkoriTM (Crizotinib), a Potent and Selective Dual Inhibitor of MET and ALK for Cancer Treatment Case History: Vemurafenib, a Potent, Selective, and First-in-Class Inhibitor of Mutant BRAF for the Treatment of Metastatic Melanoma New Chemical Entities Entering Phase III Trials in 2012 28. To Market, to Market-2012

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v. 49 ISBN 9780128001677

内容説明

Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry with an emphasis on emerging topics in the biological sciences that are expected to provide the basis for entirely new future therapies.

目次

A Personal Essay: My Experiences in the Pharmaceutical Industry Adventures in Medicinal Chemistry - A Career in Drug Discovery Natural and Synthetic Neuroactive Steroid (NAS) Modulators of GABAA and NMDA Receptors Development of LRRK2 Kinase Inhibitors for Parkinson's Disease Stimulating Neurotrophin Receptors in the Treatment of Neurodegenerative Disorders Small Molecule Modulators of GPR40 (FFA1) Recent Advances in the Development of P2Y12 Receptor Antagonists as Antiplatelet Agents Current Approaches to the Treatment of Atrial Fibrillation Advances in the Discovery of Small Molecule IRAK4 Inhibitors H4 Receptor Antagonists and Their Potential Therapeutic Applications Urate Crystal Deposition Disease and Gout - New Therapies for an Old Problem p53 - MDM2 and MDMX Antagonists Modulators of Atypical Protein Kinase C as Anticancer Agents Advancement of Cell Wall Inhibitors in Mycobacterium Tuberculosis Nucleosides and Nucleotides for the Treatment of Viral Diseases Advances in Inhibitors of Penicillin Binding Proteins and ss-lactamases as Antibacterial Agents Tumor Microenvironment as Target in Cancer Therapy Novel Screening Paradigms for the Identification of Allosteric Modulators and /or Biased Ligands for Challenging G-Protein-Coupled Receptors (GPCRs) Mer Tyrosine Kinase Receptor: Therapeutic Opportunities in Oncology, Virology and Cardiovascular Indications Disease Modifying Agents for the Treatment of Cystic Fibrosis Advancements in Stapled Peptide Drug Discovery and Development Cytochrome P450 Enzyme Metabolites in Lead Discovery and Development Case History: ForxigaTM (Dapagliflozin), a Potent Selective SGLT2 Inhibitor for Treatment of Diabetes Case History: Kalydeco (R) (VX-770, Ivacaftor), a CFTR Potentiator for the Treatment of Patients with Cystic Fibrosis and the G551D-CFTR Mutation Case History: XeljanzTM (Tofacitinib Citrate), A First-In-Class Janus Kinase (JAK) Inhibitor for the Treatment of Rheumatoid Arthritis New Chemical Entities Entering Phase III Trials in 2013 To Market, To Market - 2013

巻冊次

v. 50 ISBN 9780128130698

内容説明

Platform Technologies in Drug Discovery and Validation, Volume 50, the latest release in the Annual Reports in Medicinal Chemistry series, provides timely and critical reviews of important topics in medicinal chemistry, with an emphasis on emerging topics in the biological sciences. Topics covered in this new volume include DELT, Oligos: ASO, siRNA, CRISPR, Micro-fluidic chemistry, High throughput screening, Kinase-centric computational drug development, Virtual Screening, Phenotypic screening, PROTACS, Chemical Biology, Fragment-based lead generation, Antibody-Drug Conjugates, Antibody-recruiting small molecules, Deuteration, and Peptides.

目次

1. DNA-Encoded Library Technology: A Brief Guide to Its Evolution and Impact on Drug Discovery Robert A. Goodnow Jr. and Christopher P. Davie 2. The Chemistry of Oligonucleotide Delivery David B. Rozema 3. CRISPR–Cas9 for Drug Discovery in Oncology Sylvie M. Guichard 4. Recent Advances of Microfluidics Technologies in the Field of Medicinal Chemistry László Ürge, Jesus Alcazar, Lena Huck and György Dormán 5. High-Throughput Screening Mary Jo Wildey, Anders Haunso, Matthew Tudor, Maria Webb and Jonathan H. Connick 6. Kinase-Centric Computational Drug Development Albert J. Kooistra and Andrea Volkamer 7. Free Energy Calculation Guided Virtual Screening of Synthetically Feasible Ligand R-Group and Scaffold Modifications: An Emerging Paradigm for Lead Optimization Robert Abel and Sathesh Bhat 8. Phenotypic Screening Alleyn T. Plowright and Lauren Drowley 9. Targeted Protein Degradation Nello Mainolfi and Tim Rasmusson 10. Chemical Biology in Drug Discovery M. Paola Castaldi, Andrea Zuhl, Piero Ricchiuto and J. Adam Hendricks 11. Fragment-Based Lead Discovery Ben J. Davis and Stephen D. Roughley 12. Antibody-Drug Conjugates Amit Kumar, Jason White, R. James Christie, Nazzareno Dimasi and Changshou Gao 13. Antibody-Recruiting Small Molecules: Synthetic Constructs as Immunotherapeutics Patrick J. McEnaney, Christopher G. Parker and Andrew X. Zhang 14. A Decade of Deuteration in Medicinal Chemistry Julie F. Liu, Scott L. Harbeson, Christopher L. Brummel, Roger Tung, Robert Silverman and Dario Doller 15. From Natural Peptides to Market Claudio D. Schteingart and Jolene L. Lau

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v. 51 ISBN 9780128151433

内容説明

Neglected Diseases: Extensive Space for Modern Drug Discovery provides in-depth reviews on the last progresses about neglected tropical diseases research. Topics covered in this volume include Leishmaniasis, Tripanosomiasis, Onchocerciasis and Ebolavirus infections, with insights on the future of the research on them. Part of the volume is devoted to recent contributions this field received from X-Ray crystallography.

目次

1. Targeting Human Onchocerciasis: Recent Advances Beyond Ivermectin Stefano Sainas, Franco Dosio, D. Boschi and M.L. Lolli 2. Scaffolds and Biological Targets Avenue to Fight Against Drug Resistance in Leishmaniasis Chiara Borsari, Antonio Quotadamo, Stefania Ferrari, A. Venturelli, Anabela Cordeiro, Nuno Santarem and Maria Paola Costi 3. Drugs and Drug Resistance in African and American Trypanosomiasis Jaime Franco, Laura Scarone and Marcelo A. Comini 4. Antiviral Agents Against Ebola Virus Infection: Repositioning Old Drugs and Finding Novel Small Molecules Elisa Fanunza, Aldo Frau, Angela Corona and Enzo Tramontano 5. X-Ray Crystallography Contributions to Drug-Discovery Against Parasite Infections Cecilia Pozzi, Giusy Tassone and Stefano Mangani

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v. 52 ISBN 9780128175569

内容説明

Some of the more recent efforts in tuberculosis (TB) and trypanosomiasis drug discovery from both Product Development Partnerships (PDPs) and academia are highlighted in this this volume. Drug discovery approaches include both target- and phenotypic whole cell screening- approaches. Regarding the latter, mechanism of action studies through target identification are also illustrated.

目次

1. Tuberculosis Steven J. Berthel, Christopher B. Cooper and Nader P. Fotouhi 2. Antituberculosis agents: Beyond medicinal chemistry rules Marco Pieroni 3. Development of MmpL3 inhibitors for tuberculosis treatment Giovanna Poce, Sara Consalvi, Giulia Venditti, Cristina Scarpecci and Mariangela Biava 4. Inhibitors of enzymes in the electron transport chain of Mycobacterium tuberculosis Andrew M. Thompson and William A. Denny 5. Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance Nicolas Willand, Marion Flipo, Baptiste Villemagne, Alain Baulard and Benoit Deprez 6. Sustainable anti-trypanosomatid drugs: An aspirational goal for medicinal chemistry Maria Laura Bolognesi

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v. 53 ISBN 9780128198667

内容説明

Medicinal Chemistry Approaches to Malaria and Other Tropical Disease, Volume 53 in the Annual Reports in Medicinal Chemistry series, highlights new advances in the field, with this new volume presenting interesting chapters. Each chapter is written by an international board of authors.

目次

1. A decade of malaria phenotypic screenings: Key lessons on the discovery and development of new antimalarial drugs Esther Fernandez, Maria Isabel Castellote, Maria Jesus Chaparro, Beatriz Diaz, Jorge Fernandez, Mariola Gordo, Laura de las Heras, Maria Luisa Leon, Lourdes Rueda and Felix Calderon 2. Medicinal chemistry progression of antimalarial hits from phenotypic whole cell screening of SoftFocus libraries Peter M. Cheuka, Godfrey Mayoka, John Okombo and Kelly Chibale 3. The hybrid antimalarial approach Princy Gupta, Lovepreet Singh and Kamaljit Singh 4. Dealing with schistosomiasis: Current drug discovery strategies Sandra Gemma, Stefano Federico, Simone Brogi, Margherita Brindisi, Stefania Butini and Giuseppe Campiani 5. Shortcuts to schistosomiasis drug discovery: The state-of-the-art Jose T. Moreira-Filho, Rafael F. Dantas, Mario R. Senger, Arthur C. Silva, Dulcinea M. B. Campos, Eugene Muratov, Floriano P. Silva-Junior, Carolina H. Andrade and Bruno J. Neves 6. Multicomponent reactions: A mighty journey partner for infectious tropical disease drug discovery Diego Munoz-Torrero, Rodolfo Lavilla, F. Javier Perez-Areales and Ouldouz Ghashghaei

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詳細情報

• NII書誌ID(NCID): BA11402484
• ISBN:
  • 0120405016
  • 0120405024
  • 0120405032
  • 0120405040
  • 0120405059
  • 0120405067
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  • 0120405415
  • 9780123739124
  • 9780123743442
  • 9780123747662
  • 9780123809025
  • 9780123860095
  • 9780123964922
  • 9780124171503
  • 9780128001677
  • 9780128130698
  • 9780128151433
  • 9780128175569
  • 9780128198667
• LCCN: 66026843
• 出版国コード: us
• タイトル言語コード: eng
• 本文言語コード: eng
• 出版地: New York
• ページ数/冊数: v.
• 大きさ: 26 cm
• 分類:
  • NDC8 : 491.4