2,4-Thiazolidinediones as potent and selective human beta3 agonists

  • Bioorg Med Chem Lett. 2001 Mar 26;11(6):757-60. doi: 10.1016/s0960-894x(01)00063-4.
B Hu  1 ,  J Ellingboe ,  I Gunawan ,  S Han ,  E Largis ,  Z Li ,  M Malamas ,  R Mulvey ,  A Oliphant ,  F W Sum ,  J Tillett ,  V Wong
Affiliations
  • 1. Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. [email protected]
PMID: 11277513 DOI: 10.1016/s0960-894x(01)00063-4
Abstract

Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50=0.01 microM, IA=1.19) and selective (more than 110-fold over beta1 and beta2 agonist activity) beta3 agonist. This compound has also been proven to be active and selective in an in vivo mode.