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Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors
- Authors
- Kim, Se Hoan; Ramu, Ravirala; Kwon, Sung Wook; Lee, Su-Hee; Kim, Chi Hyun; Kang, Seung Kyu; Rhee, Sang Dal; Bae, Myung Ae; Ahn, Sung Hoon; Ha, Duck Chan; Cheon, Hyae Gyeong; Kim, Ki Young; Ahn, Jin Hee
- Issue Date
- 1-2월-2010
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- 11 beta-Hydroxysteroid dehydrogenase 1; Cyclic sulfonamide; Diabetes; Inhibitor
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.20, no.3, pp.1065 - 1069
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 20
- Number
- 3
- Start Page
- 1065
- End Page
- 1069
- ISSN
- 0960-894X
- Abstract
- A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11 beta-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11 beta-HSD2. (C) 2009 Elsevier Ltd. All rights reserved.
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