1374986-53-4Relevant articles and documents
Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators
Mao, Weiwei,Ning, Mengmeng,Liu, Zhiqing,Zhu, Qingzhang,Leng, Ying,Zhang, Ao
, p. 2982 - 2991 (2012/07/14)
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 levels on imprinting control region (ICR) mice. Unfavorable pharmacokinetic profiles (PK) were also observed on these two compounds.