4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
2009
Abstract 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 , which demonstrated improved glycemic control, decreased serum lipids, and enhanced insulin sensitivity when dosed ip in diabetic ob/ob mice.
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