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 IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity...

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Main Authors:	Wen-Long Wang, Dong-Lin Yang, Li-Xin Gao, Chun-Lan Tang, Wei-Ping Ma, Hui-Hua Ye, Si-Qi Zhang, Ya-Nan Zhao, Hao-Jie Xu, Zhao Hu, Xia Chen, Wen-Hua Fan, Hai-Jun Chen, Jing-Ya Li, Fa-Jun Nan, Jia Li, Bainian Feng
Format:	Article
Language:	English
Published:	MDPI AG 2013-12-01
Series:	Molecules
Subjects:	1H-2,3-dihydroperimidine derivatives PTP1B inhibitors selectivity structure-activity relationships (SAR)
Online Access:	http://www.mdpi.com/1420-3049/19/1/102

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spelling	doaj-618717cae9844bf79ad9a10f3f4822f42020-11-24T22:25:04ZengMDPI AGMolecules1420-30492013-12-0119110212110.3390/molecules19010102molecules190101021H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B InhibitorsWen-Long Wang0Dong-Lin Yang1Li-Xin Gao2Chun-Lan Tang3Wei-Ping Ma4Hui-Hua Ye5Si-Qi Zhang6Ya-Nan Zhao7Hao-Jie Xu8Zhao Hu9Xia Chen10Wen-Hua Fan11Hai-Jun Chen12Jing-Ya Li13Fa-Jun Nan14Jia Li15Bainian Feng16School of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaJiangshu Alpha Biopharmaceuticals, Inc. Wuxi 214122, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaState key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, ChinaSchool of Pharmaceutical Science, Jiangnan University, Wuxi 214122, ChinaA 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.http://www.mdpi.com/1420-3049/19/1/1021H-2,3-dihydroperimidine derivativesPTP1Binhibitorsselectivitystructure-activity relationships (SAR)
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Wen-Long Wang Dong-Lin Yang Li-Xin Gao Chun-Lan Tang Wei-Ping Ma Hui-Hua Ye Si-Qi Zhang Ya-Nan Zhao Hao-Jie Xu Zhao Hu Xia Chen Wen-Hua Fan Hai-Jun Chen Jing-Ya Li Fa-Jun Nan Jia Li Bainian Feng
spellingShingle	Wen-Long Wang Dong-Lin Yang Li-Xin Gao Chun-Lan Tang Wei-Ping Ma Hui-Hua Ye Si-Qi Zhang Ya-Nan Zhao Hao-Jie Xu Zhao Hu Xia Chen Wen-Hua Fan Hai-Jun Chen Jing-Ya Li Fa-Jun Nan Jia Li Bainian Feng 1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors Molecules 1H-2,3-dihydroperimidine derivatives PTP1B inhibitors selectivity structure-activity relationships (SAR)
author_facet	Wen-Long Wang Dong-Lin Yang Li-Xin Gao Chun-Lan Tang Wei-Ping Ma Hui-Hua Ye Si-Qi Zhang Ya-Nan Zhao Hao-Jie Xu Zhao Hu Xia Chen Wen-Hua Fan Hai-Jun Chen Jing-Ya Li Fa-Jun Nan Jia Li Bainian Feng
author_sort	Wen-Long Wang
title	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
title_short	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
title_full	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
title_fullStr	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
title_full_unstemmed	1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors
title_sort	1h-2,3-dihydroperimidine derivatives: a new class of potent protein tyrosine phosphatase 1b inhibitors
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2013-12-01
description	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.
topic	1H-2,3-dihydroperimidine derivatives PTP1B inhibitors selectivity structure-activity relationships (SAR)
url	http://www.mdpi.com/1420-3049/19/1/102
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1H-2,3-Dihydroperimidine Derivatives: A New Class of Potent Protein Tyrosine Phosphatase 1B Inhibitors

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