期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 3, 页码 1065-1069出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.12.035
关键词
11 beta-Hydroxysteroid dehydrogenase 1; Cyclic sulfonamide; Diabetes; Inhibitor
资金
- Center for Biological Modulators of the 21st Century Frontier RD Program
- Ministry of Education, Science and Technology, Korea
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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