beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action

  • Bioorg Med Chem. 2007 Jul 1;15(13):4396-405. doi: 10.1016/j.bmc.2007.04.035.
Jason Xiang  1 ,  Manus Ipek ,  Vipin Suri ,  May Tam ,  Yuzhe Xing ,  Nelson Huang ,  Yanling Zhang ,  James Tobin ,  Tarek S Mansour ,  John McKew
Affiliations
  • 1. Chemical and Screening Sciences, Wyeth Research, 200 Cambridge Park Drive, MA 02140, USA. [email protected]
PMID: 17490884 DOI: 10.1016/j.bmc.2007.04.035
Abstract

The design, synthesis, and biological evaluation of beta-keto sulfones as 11beta-HSD1 inhibitors and the mechanism of inhibition are described here. This class of compounds is not active against 11beta-HSD2 and therefore may have therapeutic potential for metabolic syndrome and type 2 diabetes.