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

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.

Extensive SAR studies of a series derived from RY-337, a novel non-peptidic bombesin receptor subtype-3 (BRS-3) agonist lead, led to the discovery of compound 22e with significantly improved potency at both rodent and human BRS-3. Analogs in this series demonstrated good rat pharmacokinetics.Figure optionsDownload as PowerPoint slide