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. 2012 May 1;20(9):2982-91.
doi: 10.1016/j.bmc.2012.03.008. Epub 2012 Mar 8.

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

Weiwei Mao  1 , Mengmeng Ning, Zhiqing Liu, Qingzhang Zhu, Ying Leng, Ao Zhang
Affiliations

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

Weiwei Mao et al. Bioorg Med Chem. .

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 EC(50) 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 levels on imprinting control region (ICR) mice. Unfavorable pharmacokinetic profiles (PK) were also observed on these two compounds.

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