Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators

…, M Ning, Z Liu, Q Zhu, Y Leng, A Zhang

Index: Mao, Weiwei; Ning, Mengmeng; Liu, Zhiqing; Zhu, Qingzhang; Leng, Ying; Zhang, Ao Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 9 p. 2982 - 2991

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Citation Number: 18

Abstract

A series of benzamide derivatives were assembled by using the privileged-fragment- merging (PFM) strategy and their SAR studies as glucokinase activators were described. Compounds 5 and 16b were identified having a suitable balance of potency and activation profile. They showed EC50 values of 28.3 and 44.8 nM, and activation folds of 2.4 and 2.2, respectively. However, both compounds displayed a minor reduction in plasma glucose ...