Identification of Cyclicsulfonamide Derivatives with an Acetamide Group as 11β-Hydroxysteroid Dehydrogenase 1 Inhibitors

Se Hoan Kim; Sung Wook Kwon; So Young Chu; Jae Hong Lee; Banda Narsaiah; Chi Hyun Kim; Seung Kyu Kang; Nam Sook Kang; Sang Dal Rhee; Myung Ae Bae; Sung Hoon Ahn; Duck Chan Ha; Ki Young Kim; Jin Hee Ahn

doi:10.1248/cpb.59.46

Regular Articles

Identification of Cyclicsulfonamide Derivatives with an Acetamide Group as 11β-Hydroxysteroid Dehydrogenase 1 Inhibitors

Se Hoan Kim, Sung Wook Kwon, So Young Chu, Jae Hong Lee, Banda Narsaiah, Chi Hyun Kim, Seung Kyu Kang, Nam Sook Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Duck Chan Ha, Ki Young Kim, Jin Hee Ahn

著者情報

キーワード: diabetes, anti-diabetic agent, 11β-hydroxysteroid dehydrogenase type 1, cyclic sulfonamide

ジャーナルフリー

2011 年 59 巻 1 号 p. 46-52

DOI https://doi.org/10.1248/cpb.59.46

詳細

抄録

In the continuation of our 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor research, cyclic sulfonamide derivatives with an acetamide group at the 2-position were synthesized and evaluated for their abilities to inhibit 11β-HSD1. Among this series, Compound 34 showed good in vitro activity toward human 11β-HSD1, selectivity against 11β-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 11β-HSD1.

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