Synthesis and Biological Evaluation of Aryl-phospho-indole as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

被引：164

作者：

Alexandre, Francois-Rene ^{[1
]}

Amador, Agnes ^{[1
]}

Bot, Stephanie ^{[1
]}

Caillet, Catherine ^{[1
]}

Convard, Thierry ^{[1
]}

Jakubik, Jocelyn ^{[3
]}

Musiu, Chiara ^{[2
]}

Poddesu, Barbara ^{[2
]}

Vargiu, Luana ^{[2
]}

Liuzzi, Michel ^{[2
]}

Roland, Arlene ^{[1
]}

Seifer, Maria ^{[3
]}

Standring, David ^{[3
]}

Storer, Richard ^{[1
]}

Dousson, Cyril B. ^{[1
]}

机构：

[1] Labs Idenix, Dept Chim Med, F-34189 Montpellier 4, France

[2] Univ Cagliari, Cooperat Lab Idenix, Zona Ind Macchiareddu UTA, Idenix Pharmaceut, I-09010 Cagliari, Italy

[3] Idenix Pharmaceut, Cambridge, MA 02139 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 54卷 / 01期

关键词：

ANALOGS; DESIGN; POTENT;

D O I：

10.1021/jm101142k

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 3-aryl-phospho-indole (API) non-nucleoside reverse transcriptase inhibitors of HIV-1 was developed Chemical variation in the phosphorus linker led to the discovery of 3-phenyl-methyl-phosphinate-2-carboxamide 14, which possessed excellent potency against wild-type HIV-1 as well as viruses bearing K103N and Y181C single mutants in the reverse transcriptase gene Chiral separation of the enantiomers showed that only R enantiomer retained the activity The pharmacokinetic, solubility, and metabolic properties of 14 were assessed

引用

页码：392 / 395

页数：4

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