4-(Phenylsulfonamidomethyl) benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice

X Zhang, Z Zhou, H Yang, J Chen, Y Feng, L Du…

文献索引：Zhang, Xu; Zhou, Zhou; Yang, Huaiyu; Chen, Junhua; Feng, Ying; Du, Lili; Leng, Ying; Shen, Jianhua Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 15 p. 4455 - 4458

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被引用次数: 14

摘要

Selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential as treatments for type 2 diabetes. Presented herein are the syntheses, structure–activity relationships, and efficacy evaluation of 4-( phenylsulfonamidomethyl) benzamides as 11β-HSD1 inhibitors. Through modification of our initial lead 5, we have identified potent and selective 11β-HSD1 inhibitors, such as 11n, ...