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

Bioorg Med Chem Lett 2010 Mar 4;20(6):1913-7. Epub 2010 Feb 4.

Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.

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.

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http://dx.doi.org/10.1016/j.bmcl.2010.01.154DOI Listing
March 2010
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