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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1551-4. doi: 10.1016/j.bmcl.2010.01.082. Epub 2010 Jan 25.

Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors.

Author information

1
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. unmesh.shah@spcorp.com

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.

PMID:
20149650
DOI:
10.1016/j.bmcl.2010.01.082
[Indexed for MEDLINE]

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