Heterocyclic glucocorticoid receptor modulators with a 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core

  • Bioorg Med Chem Lett. 2013 Oct 15;23(20):5571-4. doi: 10.1016/j.bmcl.2013.08.049.
Hai-Yun Xiao  1 ,  Dauh-Rurng Wu ,  James E Sheppeck 2nd ,  Sium F Habte ,  Mark D Cunningham ,  John E Somerville ,  Joel C Barrish ,  Steven G Nadler ,  T G Murali Dhar
Affiliations
  • 1. Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543-4000, United States.
PMID: 24011644 DOI: 10.1016/j.bmcl.2013.08.049
Abstract

A series of heterocyclic Glucocorticoid Receptor (GR) modulators with 2,2-dimethyl-3-phenyl-N-(thiazol or thiadiazol-2-yl)propanamide core are described. Structure-activity relationships suggest a combination of H-bond acceptor and a 4-fluorophenyl moiety as being important structural components contributing to the Glucocorticoid Receptor binding and functional activity for this series of GR modulators.

Keywords
Dissociated steroids; Glucocorticoid receptor; Non-steroidal glucocorticoid receptor agonists; Transactivation; Transrepression.