Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors

被引：30

作者：

Hu, Liming ^{[1
]}

Zhang, Sulei ^{[1
]}

He, Xianzhuo ^{[1
]}

Luo, Zaigang ^{[1
]}

Wang, Xiaoli ^{[1
]}

Liu, Wei ^{[1
]}

Qin, Xuemei ^{[1
]}

机构：

[1] Beijing Univ Technol, Coll Life Sci & Bioengn, Beijing 100124, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2012年 / 20卷 / 01期

基金：

北京市自然科学基金;

关键词：

HIV-1; Integrase; Inhibitor; 1,3-Diketo; Polyhydroxylated aromatics; Strand transfer; VIRUS TYPE-1 INTEGRASE; ONE-POT SYNTHESIS; STRAND-TRANSFER; POLYHYDROXYLATED AROMATICS; PREVENT INTEGRATION; ACID; REPLICATION; MECHANISM; NITROGEN; PLATFORM;

D O I：

10.1016/j.bmc.2011.11.014

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel beta-diketo derivatives which combined the virtues of 1,3-diketo, 1,2,3-triazole and polyhydroxylated aromatics moieties, were designed and synthesized as potential HIV-1 integrase (IN) inhibitors and evaluated their inhibition to the strand transfer process of HIV-1 integrase. The result indicates that 3,4,5-trihydroxylated aromatic derivatives exhibit good inhibition to HIV-1 integrase, but dihydroxylated aromatic derivatives and corresponding methoxy aromatic derivatives appear little inhibition to HIV-1 integrase. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：177 / 182

页数：6

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