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

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

doi:10.1248/cpb.59.46

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

Kim, Se Hoan;
Kwon, Sung Wook;
Chu, So Young;
Lee, Jae Hong;
Narsaiah, Banda;
... Ahn, Sung Hoon;
외 8명

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초록

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

키워드

diabetes anti diabetic agent; 11 beta-hydroxysteroid dehydrogenase type 1; cyclic sulfonamide; SELECTIVE INHIBITORS; METABOLIC SYNDROME; VISCERAL OBESITY; TYPE-1; MICE; DISCOVERY; 11-BETA-HSD1; OPTIMIZATION; POTENT

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

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

DOI: 10.1248/cpb.59.46

발행일: 2011-01

유형: Article

저널명: Chemical and Pharmaceutical Bulletin

권: 59

호: 1

페이지: 46 ~ 52

언어: ENG

출판사: PHARMACEUTICAL SOC JAPAN

발행국가: 일본

분량: 7 페이지

ISSN: E 1347-5223
P 0009-2363