Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4237-42. doi: 10.1016/j.bmcl.2006.05.075. Epub 2006 Jun 12.

Abstract

A series of substituted chromones were designed, synthesized, and evaluated for their ability to bind melanin-concentrating hormone receptor 1. Compounds with subnanomolar binding affinity and 66% oral bioavailability in rats were discovered.

MeSH terms

  • Administration, Oral
  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Chromones / chemical synthesis*
  • Chromones / chemistry
  • Drug Design
  • Humans
  • Melanins / chemistry*
  • Microsomes, Liver / metabolism
  • Models, Chemical
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry
  • Rats
  • Receptors, Pituitary Hormone / antagonists & inhibitors*
  • Receptors, Pituitary Hormone / chemistry*
  • Time Factors

Substances

  • Chromones
  • Melanins
  • Quinolones
  • Receptors, Pituitary Hormone
  • melanin-concentrating hormone receptor