Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists.

Michael M-C Lo,Harry R Chobanian,Oksana Palyha,Yanqing Kan,Theresa M Kelly,Xiao-Ming Guan,Marc L Reitman,Jasminka Dragovic,Kathryn A Lyons,Ravi P Nargund,Linus S Lin

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

Bombesin receptor subtype-3 (BRS-3) is an orphan G-protein coupled receptor belonging to the subfamily of bombesin-like receptors. BRS-3 is implicated in the development of obesity and diabetes. We report here small-molecule agonists that are based on a 4-(alkylamino)pyridine-3-sulfonamide core. We describe the discovery of 2a, which has mid-nanomolar potency, selectivity for human BRS-3 versus the other bombesin-like receptors, and good bioavailability.

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关键词

Bombesin receptor subtype-3 (BRS-3) agonists,Orphan G-protein coupled receptor,Pyridinesulfonylureas,Pyridinesulfonamides,Anti-obesity drugs

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