Synthesis and Protein Tyrosine Phosphatase 1B-Inhibitory Activity of Chalcones

被引：0

作者：

Zhao, Fei ^{[1
]}

Zhao, Qing-Jie ^{[1
]}

Zhang, Da-Zhi ^{[1
]}

Jin, Yong-Sheng ^{[1
]}

Zhang, Wei ^{[2
]}

机构：

[1] Second Mil Med Univ, Sch Pharm, Dept Organ Chem, Shanghai 200433, Peoples R China

[2] Second Mil Med Univ, Affiliated Changzheng Hosp, Shanghai 200003, Peoples R China

来源：

ASIAN JOURNAL OF CHEMISTRY | 2011年 / 23卷 / 12期

基金：

中国国家自然科学基金;

关键词：

Chalcones; Protein tyrosine phosphatase 1B; Inhibition; Diabetes; Obesity; INSULIN; ANALOGS; 1B;

D O I：

暂无

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of type 2 diabetes and obesity. So far less work has been conducted in the structure-activity relationship of the PTP1B inhibitory activity of chalcones. In this work, a library of 65 chalcones were synthesized and their preliminary PTP1B inhibitory activities in vitro were evaluated and reported. Among them, 27 compounds displayed good inhibitory activity on PTP1B and seven compounds showed excellent activity. These results indicate that chalcones could be used for the design of more potent PTP1B inhibitors.

引用

页码：5339 / 5342

页数：4

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