Design, synthesis, and anti-integrase activity of catechol-DKA hybrids

被引：23

作者：

Maurin, C

Bailly, F

Mbemba, G

Mouscadet, JF

Cotelle, P ^{[1
]}

机构：

[1] Univ Sci & Technol Lille, CNRS, UMR 8009, Lab Chim Organ & Macromol, F-59655 Villeneuve Dascq, France

[2] ENS Cachan, CNRS, UMR 8113, Lab Biotechnol & Pharmacol Genet Appl, F-94235 Cachan, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 09期

关键词：

antiviral; HIV-1 integrase inhibitors; DKA; catechols;

D O I：

10.1016/j.bmc.2005.12.039

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：

Following the discovery of diketoacid-containing compounds as HIV-1 integrase (IN) inhibitors, a plethora of new molecules have been published leading to four drugs under clinical trial. In an attempt to rationally design new dimeric diketoacids (DKAs) targeting two divalent metal ions on the active site of IN, potent inhibitors against purified IN were found with varied selectivity for strand transfer. In this context, we designed and synthesized a new series of catechol-DKA hybrids. These compounds presented micromolar anti-integrase activities with moderate antiviral properties. (c) 2005 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2978 / 2984

页数：7

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