Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5234-6. doi: 10.1016/j.bmcl.2005.08.043. Epub 2005 Oct 3.

Abstract

Herein, we report the discovery of the potent and selective biaryl diamide derived MCH-R1 receptor antagonist 1, which was identified upon modification of a previously disclosed biaryl urea series. This paper describes one of the strategies incorporated to remove the highly mutagenic biarylaniline present in an otherwise promising biaryl urea series.

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry*
  • Amides / pharmacology*
  • Humans
  • Receptors, Somatostatin / antagonists & inhibitors*
  • Structure-Activity Relationship
  • Urea / chemistry

Substances

  • Amides
  • MCHR1 protein, human
  • Receptors, Somatostatin
  • Urea