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Identification of Cyclicsulfonamide Derivatives with an Acetamide Group as 11 beta-Hydroxysteroid Dehydrogenase 1 Inhibitors
- Authors
- 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
- Issue Date
- Jan-2011
- Publisher
- PHARMACEUTICAL SOC JAPAN
- Keywords
- diabetes anti diabetic agent; 11 beta-hydroxysteroid dehydrogenase type 1; cyclic sulfonamide
- Citation
- CHEMICAL & PHARMACEUTICAL BULLETIN, v.59, no.1, pp.46 - 52
- Indexed
- SCIE
SCOPUS
- Journal Title
- CHEMICAL & PHARMACEUTICAL BULLETIN
- Volume
- 59
- Number
- 1
- Start Page
- 46
- End Page
- 52
- ISSN
- 0009-2363
- Abstract
- 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
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