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… - Bioorganic & medicinal …, 2009 - Elsevier
X Zhang, Z Zhou, H Yang, J Chen, Y Feng, L Du, Y Leng, J Shen
Bioorganic & medicinal chemistry letters, 2009•ElsevierSelective 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 …
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 …
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.
Elsevier
