2. Academic Validation
  3. BMS-201620: a selective beta 3 agonist

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

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543, USA. william.washburn@bms.com
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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