DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITY EVALUATION OF 2-MERCAPTO-4(3H)-QUINAZOLINONE DERIVATIVES AS NOVEL INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B

被引：8

作者：

Li, Hui ^{[1
]}

Wang, Jin-Ping ^{[1
]}

Yang, Fan ^{[1
]}

Liu, Ting ^{[1
]}

Qiu, Wen-Wei ^{[2
]}

Li, Jing-Ya ^{[3
]}

Li, Jia ^{[3
]}

Tang, Jie ^{[1
]}

机构：

[1] E China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China

[2] E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China

[3] Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, Shanghai 201203, Peoples R China

来源：

HETEROCYCLES | 2012年 / 85卷 / 08期

基金：

中国国家自然科学基金;

关键词：

PTP1B; TCPTP; Quinazolinone; Inhibition; Synthesis; QUINAZOLINONE DERIVATIVES; INSULIN SENSITIVITY; SIGNAL-TRANSDUCTION; AGENTS; PTP1B; DISCOVERY; RECEPTOR; OBESITY; COMPLEX; POTENT;

D O I：

10.3987/COM-12-12477

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of novel 2-mercapto-4(3H)-quinazolinone derivatives have been synthesized and their inhibitory effects on PTP1B and TCPTP are evaluated for the first time. Most of these derivatives showed good inhibitory activity on PTP1B and reasonable selectivity for PTP1B over TCPTP, among them 32 was the most potent PTP1B inhibitor (IC50 = 1.50 mu g/mL), and 27 possessed the best selectivity of 3.0-fold.

引用

页码：1897 / 1911

页数：15

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