%0 Journal Article
%T 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
%A Wen-Long Wang
%A Dong-Lin Yang
%A Li-Xin Gao
%A Chun-Lan Tang
%A Wei-Ping Ma
%A Hui-Hua Ye
%A Si-Qi Zhang
%A Ya-Nan Zhao
%A Hao-Jie Xu
%A Zhao Hu
%A Xia Chen
%A Wen-Hua Fan
%A Hai-Jun Chen
%A Jing-Ya Li
%A Fa-Jun Nan
%A Jia Li
%A Bainian Feng
%J Molecules
%D 2014
%I MDPI AG
%R 10.3390/molecules19010102
%X 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 4 6 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.
%K 1H-2
%K 3-dihydroperimidine derivatives
%K PTP1B
%K inhibitors
%K selectivity
%K structure-activity relationships (SAR)
%U http://www.mdpi.com/1420-3049/19/1/102