TY - JOUR
T1 - 4-(Phenylsulfonamidomethyl)benzamides as potent and selective inhibitors of the 11β-hydroxysteroid dehydrogenase type 1 with efficacy in diabetic ob/ob mice
AU - Zhang, Xu
AU - Zhou, Zhou
AU - Yang, Huaiyu
AU - Chen, Junhua
AU - Feng, Ying
AU - Du, Lili
AU - Leng, Ying
AU - Shen, Jianhua
PY - 2009/8/1
Y1 - 2009/8/1
N2 - 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. Crown
AB - 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. Crown
KW - 11β-HSD1 inhibitors
KW - 4-(Phenylsulfonamidomethyl)benzamide
KW - Type 2 diabetes
UR - https://www.scopus.com/pages/publications/67650178262
U2 - 10.1016/j.bmcl.2009.05.033
DO - 10.1016/j.bmcl.2009.05.033
M3 - 文章
C2 - 19564108
AN - SCOPUS:67650178262
SN - 0960-894X
VL - 19
SP - 4455
EP - 4458
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 15
ER -
