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

Silvia Frutos; Teresa Tarrago; Ernest Giralt

doi:10.1016/j.bmcl.2006.02.031

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

Bioorg Med Chem Lett. 2006 May 15;16(10):2677-81. doi: 10.1016/j.bmcl.2006.02.031. Epub 2006 Mar 6.

Authors

Silvia Frutos¹, Teresa Tarrago, Ernest Giralt

Affiliation

¹ Institut de Recerca Biomèdica (IRB-PCB), Parc Científic de Barcelona, Josep Samitier, 1-5. E-08028 Barcelona, Spain.

PMID: 16517158
DOI: 10.1016/j.bmcl.2006.02.031

Abstract

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 (19)F NMR for the evaluation of the inhibitory activity of new compounds against HIV-1 protease.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Binding Sites
Chromatography, High Pressure Liquid
HIV Protease / drug effects
HIV Protease Inhibitors / chemistry
HIV Protease Inhibitors / pharmacology*
HIV-1 / enzymology*
Magnetic Resonance Spectroscopy / methods*
Mass Spectrometry

Substances

HIV Protease Inhibitors
HIV Protease