Acta Pharmaceutica Sinica B (Oct 2011)

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

  • 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

DOI
https://doi.org/10.1016/j.apsb.2011.07.002
Journal volume & issue
Vol. 1, no. 3
pp. 166 – 171

Abstract

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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.

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