Bile acid conjugates of a nonsteroidal glucocorticoid receptor modulator

  • Bioorg Med Chem Lett. 2004 Aug 16;14(16):4179-83. doi: 10.1016/j.bmcl.2004.06.022.
Noah Tu  1 ,  J T Link ,  Bryan K Sorensen ,  Maurice Emery ,  Marlena Grynfarb ,  Annika Goos-Nilsson ,  Bach Nguyen
Affiliations
  • 1. Metabolic Disease Research, Abbott Laboratories, Dept 4CB, Building AP-10, Rm. L-14, 100 Abbott Park Road, Abbott Park, IL 60064-6098, USA.
PMID: 15261266 DOI: 10.1016/j.bmcl.2004.06.022
Abstract

Bile acid conjugates of a selective nonsteroidal Glucocorticoid Receptor modulator were prepared and evaluated. Potent GR binding conjugates that showed improved metabolic stability were discovered. However, cellular potency and pharmacokinetics were not substantially improved.