Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.

Bioorg Med Chem Lett 2010 May 12;20(9):2912-5. Epub 2010 Mar 12.

AMRI, 26 Corporate Circle, Albany, NY 12212, USA.

SAR around non-peptidic potent bombesin receptor subtype-3 (BRS-3) agonist lead 2 is presented. Attempts to replace the carboxylic acid with heterocyclic isosteres to improve oral bioavailability and brain penetration are described.

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http://dx.doi.org/10.1016/j.bmcl.2010.03.028DOI Listing
May 2010
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