Linker-modified quinoline derivatives targeting HIV-1 integrase:: synthesis and biological activity

被引：100

作者：

Bernard, C

Zouhiri, F

Normand-Bayle, M

Danet, M

Desmaële, D

Leh, H

Mouscadet, JF

Mbemba, G

Thomas, CM

Bonnenfant, S

Le Bret, M

d'Angelo, J

机构：

[1] CNRS, UMR 8076, Ctr Etud Pharmaceut Chim Organ, F-92296 Chatenay Malabry, France

[2] BioAlliance Pharma, F-75015 Paris, France

[3] Ecole Normale Super, CNRS, UMR 8113, F-94235 Cachan, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 10期

关键词：

antivirals; enzyme inhibitors; quinolines; amides; ureas;

D O I：

10.1016/j.bmcl.2004.03.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an ancillary aromatic ring linked by functionalized spacers such as amide, hydrazide, urea and 1-hydroxyprop-l-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments. (C) 2004 Elsevier Ltd. All rights reserved.

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收藏

页码：2473 / 2476

页数：4

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