Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives

The development of novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosterism principle, two novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives have been des...

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Detalles Bibliográficos
Autores principales: Jiang, Xiaofei, Zhan, Peng, Liu, Xinyong, Clercq, Erik de
Formato: Articulo Comunicacion
Lenguaje:Inglés
Publicado: 2012
Materias:
Farmacia
Antiviral activity
HIV-1
Synthesis
Thiadiazole
Thioacetanilides
Agentes Antivirales
Tiadiazoles
Acceso en línea:http://sedici.unlp.edu.ar/handle/10915/20230
http://www.latamjpharm.org/resumenes/31/5/LAJOP_31_5_2_3.pdf
Aporte de:
SEDICI (UNLP) de Universidad Nacional de La Plata
id I19-R120-10915-20230
record_format dspace
institution Universidad Nacional de La Plata
institution_str I-19
repository_str R-120
collection SEDICI (UNLP)
language Inglés
topic Farmacia
Antiviral activity
HIV-1
Synthesis
Thiadiazole
Thioacetanilides
Agentes Antivirales
Tiadiazoles
spellingShingle Farmacia
Antiviral activity
HIV-1
Synthesis
Thiadiazole
Thioacetanilides
Agentes Antivirales
Tiadiazoles
Jiang, Xiaofei
Zhan, Peng
Liu, Xinyong
Clercq, Erik de
Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
topic_facet Farmacia
Antiviral activity
HIV-1
Synthesis
Thiadiazole
Thioacetanilides
Agentes Antivirales
Tiadiazoles
description The development of novel HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating novel structures of increased potency. Based on the bioisosterism principle, two novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives have been designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. The results indicate that these compounds show good activities against HIV-1. Especially, compound 9B (EC50 = 0.019 μM) was more effective than the reference drugs nevirapine and delavirdine.
format Articulo
Comunicacion
author Jiang, Xiaofei
Zhan, Peng
Liu, Xinyong
Clercq, Erik de
author_facet Jiang, Xiaofei
Zhan, Peng
Liu, Xinyong
Clercq, Erik de
author_sort Jiang, Xiaofei
title Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
title_short Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
title_full Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
title_fullStr Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
title_full_unstemmed Synthesis and Anti-HIV Activity Evaluation of 2-(5-(Naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides Derivatives
title_sort synthesis and anti-hiv activity evaluation of 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-n-acetamides derivatives
publishDate 2012
url http://sedici.unlp.edu.ar/handle/10915/20230
http://www.latamjpharm.org/resumenes/31/5/LAJOP_31_5_2_3.pdf
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AT zhanpeng synthesisandantihivactivityevaluationof25naphthalen1yl123thiadiazol4ylthionacetamidesderivatives
AT liuxinyong synthesisandantihivactivityevaluationof25naphthalen1yl123thiadiazol4ylthionacetamidesderivatives
AT clercqerikde synthesisandantihivactivityevaluationof25naphthalen1yl123thiadiazol4ylthionacetamidesderivatives
bdutipo_str Repositorios
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