Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity

被引：18

作者：

Benjahad, Abdellah

Oumouch, Said

Guillemont, Jerome

Pasquier, Elisabeth

Mabire, Dominique

Andries, Koen

Nguyen, Chi Hung

Grierson, David S.

机构：

[1] Inst Curie, UMR CNRS 176, Lab Pharmacochim, Sect Rech,Ctr Univ, F-91405 Orsay, France

[2] Johnson & Johnson Pharmaceut Res & Dev, Med Chem Dept, Val De Reuil, France

[3] Johnson & Johnson Pharmaceut Res & Dev, Virol Drug Discovery, B-2340 Beerse, Belgium

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 03期

关键词：

NNRTI; pyridinone; IOPY; anti-HIV;

D O I：

10.1016/j.bmcl.2006.10.082

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

As part of a systematic SAR study on the 3-iodo-4-phenoxypyridinone 3 (IOPY) type non-nucleoside reverse transcriptase inhibitors, the analogues 4a-4z bearing different C-3 substituents were synthesized and evaluated for their anti-HIV activity against wild-type HIV-1 and four of the principal HIV mutant strains (K103N, Y181C, Y188L, and 1100L). The results show that the 3-vinyl analogue 4j is the only compound which displays anti-HIV activity comparable to IOPY 3, and in this respect represents a possible back-up to this lead molecule. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：712 / 716

页数：5

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