Novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives as dual-action hypoglycemic agents that activate GK and PPARγ

oleh: Hui-peng Song, Kang Tian, Lei Lei, Zhu-fang Shen, Shou-xin Liu, Li-juan Zhang, Hong-rui Song, Xiao-feng Jin, Zhi-qiang Feng

Format: Article
Diterbitkan: Elsevier 2011-10-01

Deskripsi

A series of novel N-(pyrimidin-4-yl)thiazol-2-amine derivatives have been synthesized and evaluated as glucokinase (GK) activators. Ethyl 2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl-amino)thiazole-5-carboxylate was found to be a potent dual-acting hypoglycemic agent activating both GK and PPARγ. When given orally to normal mice, the compound demonstrated significant efficacy in decreasing the glucose level after oral glucose loading.