1H-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.

نویسندگان

  • Wen-Long Wang
  • Dong-Lin Yang
  • Li-Xin Gao
  • Chun-Lan Tang
  • Wei-Ping Ma
  • Hui-Hua Ye
  • Si-Qi Zhang
  • Ya-Nan Zhao
  • Hao-Jie Xu
  • Zhao Hu
  • Xia Chen
  • Wen-Hua Fan
  • Hai-Jun Chen
  • Jing-Ya Li
  • Fa-Jun Nan
  • Jia Li
  • Bainian Feng
چکیده

A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.

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عنوان ژورنال:
  • Molecules

دوره 19 1  شماره 

صفحات  -

تاریخ انتشار 2013