Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7. doi: 10.1016/j.bmcl.2010.01.154. Epub 2010 Feb 4.

Abstract

We report SAR studies on a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead series derived from high-throughput screening hit RY-337. This effort led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3.

MeSH terms

  • Animals
  • Biological Availability
  • Drug Discovery*
  • Humans
  • Imidazoles / chemistry*
  • Imidazoles / pharmacokinetics
  • Imidazoles / pharmacology*
  • Rats
  • Receptors, Bombesin / agonists*
  • Structure-Activity Relationship

Substances

  • Imidazoles
  • Receptors, Bombesin
  • bombesin receptor subtype 3