Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase

…, Q Zhu, J Liu, L Chen, Y Leng, H Jiang, H Liu

Index: Zhang, Lei; Li, Honglin; Zhu, Qingzhang; Liu, Jun; Chen, Ling; Leng, Ying; Jiang, Hualiang; Liu, Hong Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 20 p. 7301 - 7312

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Citation Number: 22

Abstract

A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure–activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC50 of 8.95 μM and activated GK with an EC50 of 1.87 μM. The ...