Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6237-40. doi: 10.1016/j.bmcl.2009.08.076. Epub 2009 Aug 26.

Abstract

This Letter describes optimization of ghrelin receptor antagonists and inverse agonists starting from a screening hit.

MeSH terms

  • Animals
  • Anti-Obesity Agents / chemical synthesis
  • Anti-Obesity Agents / chemistry*
  • Anti-Obesity Agents / pharmacology
  • Benzenesulfonamides
  • Cell Line
  • Drug Design
  • Drug Inverse Agonism
  • Humans
  • Male
  • Obesity / drug therapy
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Ghrelin / antagonists & inhibitors*
  • Receptors, Ghrelin / metabolism
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry*
  • Sulfonamides / pharmacology

Substances

  • Anti-Obesity Agents
  • Receptors, Ghrelin
  • Sulfonamides