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

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 IC(50) values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivi...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271978/
https://www.ncbi.nlm.nih.gov/pubmed/24366088
http://dx.doi.org/10.3390/molecules19010102
Descripción
Sumario: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 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 compounds for the design of inhibitors of PTP1B as well as other PTPs.

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