1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors

Molecules

Wen-Long Wang¹  Dong-Lin Yang¹  Li-Xin Gao³  Chun-Lan Tang³  Wei-Ping Ma³  Hui-Hua Ye¹  Si-Qi Zhang¹  Ya-Nan Zhao¹  Hao-Jie Xu¹  Zhao Hu¹  Xia Chen¹  Wen-Hua Fan²  Hai-Jun Chen³  Jing-Ya Li³  Fa-Jun Nan³  Jia Li³ 

[1] School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, China; E-Mails:;Jiangshu Alpha Biopharmaceuticals, Inc. Wuxi 214122, China; E-Mail:;State key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China; E-Mails:

关键词: 1H-2;    3-dihydroperimidine derivatives;    PTP1B;    inhibitors;    selectivity;    structure-activity relationships (SAR);   

DOI  :  10.3390/molecules19010102

来源: mdpi

【 摘 要 】

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.

【 授权许可】

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© 2013 by the authors; licensee MDPI, Basel, Switzerland.