Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors

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• 作者：Se Hoan Kim ; Ravirala Ramu ; Sung Wook Kwon ; Su-Hee Lee ; Chi Hyun Kim ; Seung Kyu Kang ; Sang Dal Rhee ; Myung Ae Bae ; Sung Hoon Ahn ; Duck Chan Ha ; Hyae Gyeong Cheon ; Ki Young Kim ; Jin Hee Ahn
• 关键词：11β ; -Hydroxysteroid dehydrogenase 1 ; Cyclic sulfonamide ; Diabetes ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 February 2010
• 年：2010
• 卷：20
• 期：3
• 页码：1065-1069
• 全文大小：1411 K

文摘

A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-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 11β-HSD2.