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BMS-201620: a selective beta 3 agonist |
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| Authors: | Washburn W N Sun C-Q Bisacchi G Wu G Cheng P T Sher P M Ryono D Gavai A V Poss K Girotra R N McCann P J Mikkilineni A B Dejneka T C Wang T C Merchant Z Morella M Arbeeny C M Harper T W Slusarchyk D A Skwish S Russell A D Allen G T Tesfamariam B Frohlich B H Abboa-Offei B E Cap M Waldron T L George R J Young D Dickinson K E Seymour A A |
| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. william.washburn@bms.com |
| Abstract: | A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation. |
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