Synthesis and Biological Evaluation of Quinolone Acid Derivatives Having Polyhydroxylated Aromatics as HIV-1 Integrase Inhibitions

被引：5

作者：

Xu, Xuemei ^{[1
]}

Luo, Zaigang ^{[1
]}

He, Kuai ^{[1
]}

Zhang, Mingyang ^{[1
]}

机构：

[1] AnHui Univ Sci & Technol, Coll Chem Engn, Huainan 232001, Anhui, Peoples R China

来源：

ADVANCES IN CHEMICAL, MATERIAL AND METALLURGICAL ENGINEERING, PTS 1-5 | 2013年 / 634-638卷

关键词：

HIV-1; integrase inhibitors; quinolone acid; polyhydroxylated aromatic; strand transfer; NITROGEN;

D O I：

10.4028/www.scientific.net/AMR.634-638.1116

中图分类号：

TQ [化学工业];

学科分类号：

0817 ;

摘要：

A small chemical library of quinolone acid derivatives were synthesized as potential HIV-1 integrase inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. Their structures were characterized by NMR, MS and HRMS. The result indicates that quinolone acid derivatives having 3,4,5-trihydroxylated aromatic substituent on the N-1 position of quinolone ring exhibit good inhibition with IC50 of 2.6 mu M.

引用

页码：1116 / 1119

页数：4

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