BMS-201620: a selective beta 3 agonist

  • Bioorg Med Chem Lett. 2004 Jul 5;14(13):3525-9. doi: 10.1016/j.bmcl.2004.04.074.
W N Washburn  1 ,  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
Affiliations
  • 1. Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. [email protected]
PMID: 15177466 DOI: 10.1016/j.bmcl.2004.04.074
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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