Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors

  • Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4. doi: 10.1016/j.bmcl.2010.01.082.
Unmesh Shah  1 ,  Craig D Boyle ,  Samuel Chackalamannil ,  Hana Baker ,  Timothy Kowalski ,  Julie Lee ,  Giuseppe Terracina ,  Lili Zhang
Affiliations
  • 1. Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
PMID: 20149650 DOI: 10.1016/j.bmcl.2010.01.082
Abstract

Inhibition of 11beta-HSD1 has demonstrated potential in the treatment of various components of metabolic syndrome. We wish to report herein the discovery of novel azabicyclic sulfonamide based 11beta-HSD1 inhibitors. Highly potent compounds exhibiting inhibitory activities at both human and mouse 11beta-HSD1 were identified. Several compounds demonstrated significant in vivo activity in the mouse cortisone challenge assay.