Synthesis and Structure–Activity Relationship of Naphtho[1,2-<i>b</i>]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists

DOI Web Site Web Site PubMed 1 Citations 6 References
  • Lim Chae Jo
    Division of Drug Discovery Research, Korea Research Institute of Chemical Technology Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology
  • Choi Jun Young
    Division of Drug Discovery Research, Korea Research Institute of Chemical Technology Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology
  • Lee Byung Ho
    Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
  • Oh Kwang-Seok
    Division of Drug Discovery Research, Korea Research Institute of Chemical Technology
  • Yi Kyu Yang
    Division of Drug Discovery Research, Korea Research Institute of Chemical Technology Department of Medicinal and Pharmaceutical Chemistry, University of Science and Technology

Bibliographic Information

Other Title
  • Synthesis and Structure-Activity Relationship of Naphtho[1,2-b]furan-2-carboxamide Derivatives as Melanin Concentrating Hormone Receptor 1 Antagonists

Search this article

Abstract

The discovery that novel naphtho[1,2-b]furan-2-carboxamides containing linked piperidinylphenylacetamide groups serve as melanin concentrating hormone receptor 1 (MCH-R1) antagonists is described. An extensive structure–activity relationship (SAR) study, probing members of this family that contain a variety of aryl and heteroaryl groups at C-5 of the naphtho[1,2-b]furan-2-carboxamide skeleton and having different chain linker lengths, led to the identification of the 5-(4-pyridinyl) substituted analog 10b as a highly potent MCH-R1 antagonist with an IC50 value of 3 nM. This substance also displays good metabolic stability and it does not significantly inhibit cytochrome P450 (CYP450) enzymes. However, 10b has unacceptable oral bioavailability.

Journal

Citations (1)*help

See more

References(6)*help

See more

Keywords

Details 詳細情報について

Report a problem

Back to top