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Published on: August 6, 2020
Azabicyclic sulfonamides as potent 11beta-HSD1 inhibitors
Unmesh Shah1, Craig D Boyle, Samuel Chackalamannil
1Merck 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.
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