Molecules p. 102 - 121 (2014)
Update date:2022-08-04
Topics:
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
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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