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

WL Wang, DL Yang, LX Gao, CL Tang, WP Ma, HH Ye…

Index: Wang, Wen-Long; Yang, Dong-Lin; Gao, Li-Xin; Tang, Chun-Lan; Ma, Wei-Ping; Ye, Hui-Hua; Zhang, Si-Qi; Zhao, Ya-Nan; Xu, Hao-Jie; Hu, Zhao; Chen, Xia; Fan, Wen-Hua; Chen, Hai-Jun; Li, Jing-Ya; Nan, Fa-Jun; Li, Jia; Feng, Bainian Molecules, 2014 , vol. 19, # 1 p. 102 - 121

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Citation Number: 2

Abstract

Abstract: A series of 1 H-2, 3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC 50 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 ...