Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to i...

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Autores principales: Famiglini, Valeria, Silvestri, Romano
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273187/
https://www.ncbi.nlm.nih.gov/pubmed/26891289
http://dx.doi.org/10.3390/molecules21020221
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author Famiglini, Valeria
Silvestri, Romano
author_facet Famiglini, Valeria
Silvestri, Romano
author_sort Famiglini, Valeria
collection PubMed
description Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to investigate the effect of chirality on the antiretroviral activity of top HIV-1 NNRTI compounds, such as nevirapine (NVP), efavirenz (EFV), alkynyl- and alkenylquinazolinone DuPont compounds (DPC), diarylpyrimidine (DAPY), dihydroalkyloxybenzyloxopyrimidine (DABO), phenethylthiazolylthiourea (PETT), indolylarylsulfone (IAS), arylphosphoindole (API) and trifluoromethylated indole (TFMI) The chiral separation, the enantiosynthesis, along with the biological properties of these HIV-1 NNRTIs, are discussed.
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spelling pubmed-62731872018-12-28 Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors Famiglini, Valeria Silvestri, Romano Molecules Review Chiral HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are of great interest since one enantiomer is often more potent than the corresponding counterpart against the HIV-1 wild type (WT) and the HIV-1 drug resistant mutant strains. This review exemplifies the various studies made to investigate the effect of chirality on the antiretroviral activity of top HIV-1 NNRTI compounds, such as nevirapine (NVP), efavirenz (EFV), alkynyl- and alkenylquinazolinone DuPont compounds (DPC), diarylpyrimidine (DAPY), dihydroalkyloxybenzyloxopyrimidine (DABO), phenethylthiazolylthiourea (PETT), indolylarylsulfone (IAS), arylphosphoindole (API) and trifluoromethylated indole (TFMI) The chiral separation, the enantiosynthesis, along with the biological properties of these HIV-1 NNRTIs, are discussed. MDPI 2016-02-16 /pmc/articles/PMC6273187/ /pubmed/26891289 http://dx.doi.org/10.3390/molecules21020221 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Famiglini, Valeria
Silvestri, Romano
Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title_full Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title_fullStr Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title_full_unstemmed Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title_short Focus on Chirality of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
title_sort focus on chirality of hiv-1 non-nucleoside reverse transcriptase inhibitors
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273187/
https://www.ncbi.nlm.nih.gov/pubmed/26891289
http://dx.doi.org/10.3390/molecules21020221
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