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Pyridinesulfonylureas and pyridinesulfonamides as selective bombesin receptor subtype-3 (BRS-3) agonists |
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| Authors: | Lo Michael M-C Chobanian Harry R Palyha Oksana Kan Yanqing Kelly Theresa M Guan Xiao-Ming Reitman Marc L Dragovic Jasminka Lyons Kathryn A Nargund Ravi P Lin Linus S |
| Affiliation: | a Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA b Department of Metabolic Disorders, Merck Research Laboratories, Rahway, NJ 07065, USA c Department of Drug Metabolism, Merck Research Laboratories, Rahway, NJ 07065, USA |
| Abstract: | 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. |
| Keywords: | Bombesin receptor subtype-3 (BRS-3) agonists Orphan G-protein coupled receptor Pyridinesulfonylureas Pyridinesulfonamides Anti-obesity drugs |
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