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

Bioorganic & Medicinal Chemistry Letters
Silvia FrutosErnest Giralt

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.

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Citations

Nov 9, 2002·Journal of Clinical Virology : the Official Publication of the Pan American Society for Clinical Virology·Joel E Gallant
Jan 28, 2009·Nature Reviews. Drug Discovery·Maurizio PellecchiaGregg Siegal
Dec 22, 2015·Analytical Biochemistry·Marina VeronesiClaudio Dalvit
Feb 18, 2012·Journal of Ethnopharmacology·Helen SheridanJandirk Sendker
Apr 17, 2010·Chembiochem : a European Journal of Chemical Biology·Nessim KichikErnest Giralt
Jun 13, 2019·Current Medicinal Chemistry·Cong Bao Kang
Feb 14, 2007·ChemMedChem·Teresa TarragoErnest Giralt
Aug 7, 2013·Chembiochem : a European Journal of Chemical Biology·Chiara LambruschiniClaudio Dalvit
Apr 30, 2020·Journal of Biomolecular NMR·Claudio DalvitAnna Vulpetti
Dec 18, 2013·ChemMedChem·Marina VeronesiClaudio Dalvit
Oct 9, 2018·Journal of Medicinal Chemistry·Claudio Dalvit, Anna Vulpetti
Sep 4, 2009·Journal of Fluorine Chemistry·David B BerkowitzChristopher D McCune
Apr 10, 2007·Journal of the American Chemical Society·Gianluca PapeoClaudio Dalvit
Nov 6, 2021·Chembiochem : a European Journal of Chemical Biology·Emmanuelle DevillersJulien Pytkowicz

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