A fast and robust 19F NMR-based method for finding new HIV-1 protease inhibitors

被引：20

作者：

Frutos, S

Tarrago, T

Giralt, E

机构：

[1] Inst Recerca Biomed IRB PCB, E-08028 Barcelona, Spain

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

F-19; NMR; HIV-1; protease; NMR screening; protease inhibitors; traditional Chinese medicine;

D O I：

10.1016/j.bmcl.2006.02.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The human immunodeficiency virus (HIV) which encodes, among other indispensable enzymes, an aspartic protease that is essential for viral maturation and replication. Numerous inhibitors of the protease have been developed. However, the eventual resistance of HIV-1 to these drugs implies a continuous battle to develop new inhibitors. Proposed herein is a robust, fast, and reliable method employing F-19 NMR for the evaluation of the inhibitory activity of new compounds against HIV-1 protease. (C) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2677 / 2681

页数：5

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