BMS-201620: a selective beta 3 agonist.
W N Washburn, C-Q Sun, G Bisacchi, G Wu, P T Cheng, P M Sher, D Ryono, A V Gavai, K Poss, R N Girotra, P J McCann, A B Mikkilineni, T C Dejneka, T C Wang, Z Merchant, M Morella, C M Arbeeny, T W Harper, D A Slusarchyk, S Skwish, A D Russell, G T Allen, B Tesfamariam, B H Frohlich, B E Abboa-Offei, M Cap, T L Waldron, R J George, D Young, K E Dickinson, A A Seymour
Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. william.washburn@bms.com
Bioorganic & medicinal chemistry letters 2004 Jul 5A 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.
Citation
W N Washburn, C-Q Sun, G Bisacchi, G Wu, P T Cheng, P M Sher, D Ryono, A V Gavai, K Poss, R N Girotra, P J McCann, A B Mikkilineni, T C Dejneka, T C Wang, Z Merchant, M Morella, C M Arbeeny, T W Harper, D A Slusarchyk, S Skwish, A D Russell, G T Allen, B Tesfamariam, B H Frohlich, B E Abboa-Offei, M Cap, T L Waldron, R J George, D Young, K E Dickinson, A A Seymour. BMS-201620: a selective beta 3 agonist. Bioorganic & medicinal chemistry letters. 2004 Jul 5;14(13):3525-9
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PMID: 15177466
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