Identification of cyclicsulfonamide derivatives with an acetamide group as 11beta-hydroxysteroid dehydrogenase 1 inhibitors

Literature Life Science

In vitro inhibition activity of 11 beta -HSD1 assessed by the HTRF cortisol assay

Abstract

In the continuation of our 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitor research, cyclic sulfonamide derivatives with an acetamide group at the 2-position were synthesized and evaluated for their abilities to inhibit 11beta-HSD1. Among this series, Compound 34 showed good in vitro activity toward human 11beta-HSD1, selectivity against 11beta-HSD2, microsomal stability, good pharmacokinetic and safety profiles human ether-a-go-go related gene (hERG and cytochrome P450 (CYP)). Also, a docking study explained the activity difference between human and mouse 11beta-HSD1.

Details

Chem Pharm Bull (Tokyo). 2011;59(1):46-52

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