Synthesis and PTP1B Inhibitory Activity of (E)-1-Substitutedphenyl-3-(4-((E)-(2-(4-phenylthiazol-2-yl)hydrazono)methyl)pheny1)-prop-2-en-1-ones

被引：6

作者：

Sun, Liangpeng ^{[1
]}

Jiang, Zhe ^{[2
]}

Gao, Lixin ^{[3
]}

Liu, Xiaofang ^{[1
]}

Quan, Yingchun ^{[1
]}

Zheng, Guanghao ^{[1
]}

Li, Jia ^{[3
]}

Piao, Huri ^{[1
]}

机构：

[1] Yanbian Univ, Coll Pharm, Minist Educ, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133002, Peoples R China

[2] Yanbian Univ Hosp, Yanji 133002, Peoples R China

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

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2013年 / 33卷 / 07期

基金：

中国国家自然科学基金;

关键词：

PTP1B inhibitor; chalcone; carboxaldehyde hydrazone; thiazole; TYROSINE-PHOSPHATASE; 1B; STRUCTURE-BASED DESIGN; CHALCONE DERIVATIVES; ANTIBACTERIAL; SPECIFICITY; DISCOVERY; POTENT; ACID;

D O I：

10.6023/cjoc201212012

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Protein tyrosine phosphatase 1B (PTP1B) has recently been identified as new drug target for type II diabetes and obesity due to that it is a negative regulator of the insulin and leptin-signaling pathway. In order to find new nonphosphonate-based pTyr mimetics, a series of novel (E)-1-phenyl-3-(44(E)-(2-(4-phenyl-thiazol-2-yl)hydrazono)methyl)phenyl)-prop-2-en-1-one (4a similar to 4n) were designed, synthesized, and evaluated for their PTP1B inhibitory activity. The results demonstrated that all compounds presented potent inhibitory activities against PTP1B, among which compound 4h exhibited most potent with IC50 value of (2.57 +/- 0.50) mu mol-L-1.

引用

页码：1496 / 1502

页数：7

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