Document Report Card

Basic Information

ID: ALA1759937

Journal: Bioorg Med Chem Lett

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

Authors: Lo MM, Chobanian HR, Palyha O, Kan Y, Kelly TM, Guan XM, Reitman ML, Dragovic J, Lyons KA, Nargund RP, Lin LS.

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.

CiteXplore: 21354793

DOI: 10.1016/j.bmcl.2011.02.011