Pharmaceuticals

著者

書誌事項

Pharmaceuticals

edited by Jürgen Dinges and Clemens Lamberth

(Bioactive heterocyclic compound classes)

Wiley-VCH, c2012

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注記

Formerly CIP Uk

Includes bibliographical references and index

内容説明・目次

内容説明

The chemistry of heterocycles is an important branch of organic chemistry. This is due to the fact that a large number of natural products, e. g. hormones, antibiotics, vitamins, etc. are composed of heterocyclic structures. Often, these compounds show beneficial properties and are therefore applied as pharmaceuticals to treat diseases or as insecticides, herbicides or fungicides in crop protection. This volume presents important pharmaceuticals. Each of the 20 chapters covers in a concise manner one class of heterocycles, clearly structuredas follows: * Structural formulas of most important examples (market products) * Short background of history or discovery * Typical syntheses of important examples * Mode of action * Characteristic biological activity * Structure-activity relationship * Additional chemistry information (e.g. further transformations, alternative syntheses, metabolic pathways, etc.) * References. A valuable one-stop reference source for researchers in academia and industry as well as for graduate students with career aspirations in the pharmaceutical chemistry.

目次

IINTRODUCTION THE SIGNIFICANCE OF HETEROCYCLES FOR PHARMACEUTICALS AND AGROCHEMICALS Introduction Heterocycles as Framework of Biologically Active Compounds Fine-Tuning the Physicochemical Properties with Heterocycles Heterocycles as Prodrugs Heterocycles as Peptidomimetics Heterocycles as Isosteric Replacement of Functional Groups Heterocycles as Isosteric Replacement of Alicyclic Rings Heterocycles as Isosteric Replacement of other Heterocyclic Rings PART I: Neurological Disorders TROPANE-BASED ALKALOIDS AS MUSCARINIC ANTAGONISTS FOR THE TREATMENT OF ASTHMA, OBSTRUCTIVE PULMONARY DISEASE, AND MOTION SICKNESS Introduction History Synthesis Mode of Action Structure?Activity Relationships MORPHINONE-BASED OPIOID RECEPTOR AGONIST ANALGESICS Introduction History Synthesis Mode of Action Structure?Activity Relationship BARBITURIC ACID-BASED GABA(A) RECEPTOR MODULATORS FOR THE TREATMENT OF SLEEP DISORDER AND EPILEPSY AND AS ANESTHETICS Introduction History Synthesis Mode of Action Structure?Activity Relationship PHENOTHIAZINE-BASED DOPAMINE D2 ANTAGONISTS FOR THE TREATMENT OF SCHIZOPHRENIA Introduction History Synthesis Mode of Action Structure?Activity Relationships ARYLPIPERAZINE-BASED 5-HT1A RECEPTOR PARTIAL AGONISTS AND 5-HT2A ANTAGONISTS FOR THE TREATMENT OF AUTISM, DEPRESSION, ANXIETY, PSYCHOSIS, AND SCHIZOPHRENIA Introduction History Synthesis Mode of Action Structure?Activity Relationship ARYLPIPERIDINE-BASED DOPAMINE D2 ANTAGONISTS/5-HT2A ANTAGONISTS FOR THE TREATMENT OF AUTISM, DEPRESSION, SCHIZOPHRENIA, AND BIPOLAR DISORDER Introduction History Synthesis Mode of Action Structure?Activity Relationship DIBENZAZEPINE-BASED SODIUM CHANNEL BLOCKERS FOR THE TREATMENT OF NEUROPATHIC PAIN Introduction History Synthesis Mode of Action Structure?Activity Relationships PART II: Cardiovascular Diseases DIHYDROPYRIDINE-BASED CALCIUM CHANNEL BLOCKERS FOR THE TREATMENT OF ANGINA PECTORIS AND HYPERTENSION Introduction History Synthesis Mode of Action Structure?Activity Relationship TETRAZOLE-BASED ANGIOTENSIN II TYPE 1 (AT1) ANTAGONISTS FOR THE TREATMENT OF HEART FAILURE AND CONGESTIVE HYPERTENSION Introduction History Synthesis Mode of Action Structure?Activity Relationship THIAZIDE-BASED DIURETICS FOR THE TREATMENT OF HYPERTENSION AND GENITOURINARY DISORDERS Introduction History Synthesis Mode of Action Structure?Activity Relationship TETRAHYDROPYRANONE-BASED HMG-COA REDUCTASE INHIBITORS FOR THE TREATMENT OF ARTERIAL HYPERCHOLESTEROLEMIA Introduction History Synthesis Mode of Action Structure?Activity Relationship PART III: Infectious Diseases ADENINE-BASED REVERSE TRANSCRIPTASE INHIBITORS AS ANTI-HIV AGENTS Introduction History Synthesis Mode of Action Structure?Activity Relationship GUANINE-BASED NUCLEOSIDE ANALOGS AS ANTIVIRAL AGENTS Introduction History Synthesis Mode of Action Structure?Activity Relationship PENICILLIN AND CEPHALOSPORIN ANTIBIOTICS Introduction History Synthesis Mode of Action Structure?Activity Relationships PART IV: Oncology PYRIMIDINE-BASED KINASE INHIBITORS IN CANCER CHEMOTHERAPY Introduction History Synthesis Mode of Action Structure?Activity Relationship BENZYL TRIAZOLE-BASED AROMATASE INHIBITORS FOR THE TREATMENT OF BREAST CANCER Introduction History Synthesis Mode of Action Structure?Activity Relationship PART V: Inflammation and Gastrointestinal Diseases ACETONIDE-BASED GLUCOCORTICOIDS FOR THE TREATMENT OF ASTHMA, SKIN INFLAMMATION AND DISEASES OF THE EYE Introduction History Synthesis Mode of Action Structure?Activity Relationship BENZIMIDAZOLE-BASED H+/K+-ATPASE INHIBITORS FOR THE TREATMENT OF GASTROESOPHAGEAL REFLUX DISEASE Introduction History Synthesis Mode of Action Structure?Activity Relationships PART VI: Metabolic Diseases THIAZOLIDINEDIONE-BASED INSULIN SENSITIZERS:PPAR-G AGONISTS FOR THE TREATMENT OF TYPE 2 DIABETES Introduction History Synthesis Mode of Action Structure?Activity Relationship INDEX

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