(E)-1-取代苯基-3-[4-((E)-(2-(4-苯基噻唑-2-基)腙)甲基)苯基]-2-丙烯-1-酮的合成及PTP1B抑制活性研究
收稿日期: 2012-12-10
修回日期: 2013-02-20
网络出版日期: 2013-03-01
基金资助
国家自然科学基金(Nos. 81160381, 81125023)资助项目.
Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)phenyl)-prop-2-en-1-ones
Received date: 2012-12-10
Revised date: 2013-02-20
Online published: 2013-03-01
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 81160381, 81125023).
孙良鹏 , 姜哲 , 高立信 , 刘晓芳 , 全迎春 , 郑光浩 , 李佳 , 朴虎日 . (E)-1-取代苯基-3-[4-((E)-(2-(4-苯基噻唑-2-基)腙)甲基)苯基]-2-丙烯-1-酮的合成及PTP1B抑制活性研究[J]. 有机化学, 2013 , 33(07) : 1496 -1502 . DOI: 10.6023/cjoc201212012
Protein tyrosine phosphatase 1B (PTP1B) has recently been identified as new drug target for type II diabetes and obesity due to that it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel (E)-1-phenyl-3-(4-((E)-(2-(4-phenyl-thiazol-2-yl)hydrazono)methyl)phenyl)-prop-2-en-1-one (4a～4n) were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compound 4h exhibited most potent with IC50 value of (2.57±0.50) μmol·L-1.
Key words： PTP1B inhibitor; chalcone; carboxaldehyde hydrazone; thiazole
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