Discovery of non-nucleoside inhibitors of HIV-1 reverse transcriptase competing with the nucleotide substrate

被引：19

作者：

Maga, Giovanni

Radi, Marco

Zanoli, Samantha

Manetti, Fabrizio

Cancio, Reynel

Huebscher, Ulrich

Spadari, Silvio

Falciani, Chiara

Terrazas, Montserrat

Vilarrasa, Jaume

Botta, Maurizio

机构：

[1] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[2] CNR, IGM, I-27100 Pavia, Italy

[3] Univ Zurich Irchel, Inst Vet Biochem & Mol Biol, CH-8092 Zurich, Switzerland

[4] Univ Barcelona, Fac Quim, Dept Quim Organ, E-08028 Barcelona, Spain

来源：

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | 2007年 / 46卷 / 11期

关键词：

HIV-1 reverse transcriptase; competitive inhibitors; drug design; enzymes; pyrimidines;

D O I：

10.1002/anie.200604165

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

How odd! A new class of non-nucleoside reverse transcriptase inhibitors with a 6-vinylpyrimidine scaffold (1) has been found to inhibit HIV-1 reverse transcriptase (RT) by competition with the nucleotide substrate after binding to the non-nucleoside inhibitor binding pocket of the enzyme. Molecular modeling studies have been performed to elucidate their peculiar behavior. (Figure Presented). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

引用

页码：1810 / 1813

页数：4

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