| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370753 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,