Cargando…

Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents

A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis H(37)Rv, with MIC values rangi...

Descripción completa

Detalles Bibliográficos
Autores principales: Ang, Wei, Lin, Yan-Ni, Yang, Tao, Yang, Jian-Zhong, Pi, Wei-Yi, Yang, Ying-Hong, Luo, You-Fu, Deng, Yong, Wei, Yu-Quan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268079/
https://www.ncbi.nlm.nih.gov/pubmed/22357321
http://dx.doi.org/10.3390/molecules17022248
_version_ 1783376207880912896
author Ang, Wei
Lin, Yan-Ni
Yang, Tao
Yang, Jian-Zhong
Pi, Wei-Yi
Yang, Ying-Hong
Luo, You-Fu
Deng, Yong
Wei, Yu-Quan
author_facet Ang, Wei
Lin, Yan-Ni
Yang, Tao
Yang, Jian-Zhong
Pi, Wei-Yi
Yang, Ying-Hong
Luo, You-Fu
Deng, Yong
Wei, Yu-Quan
author_sort Ang, Wei
collection PubMed
description A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis H(37)Rv, with MIC values ranging from 4 to 64 μg/mL. The most potent derivative 3m showed an identical MIC value of 4 μg/mL for both M. tuberculosis H(37)Rv and rifampin-resistant M. tuberculosis 261. It demonstrated no inhibitory effects against six different tumor cell lines by a MTT assay and had a good safety profile in a vero cell line, providing a good lead for subsequent optimization in search of novel affordable antitubercular agents.
format Online
Article
Text
id pubmed-6268079
institution National Center for Biotechnology Information
language English
publishDate 2012
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62680792018-12-10 Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents Ang, Wei Lin, Yan-Ni Yang, Tao Yang, Jian-Zhong Pi, Wei-Yi Yang, Ying-Hong Luo, You-Fu Deng, Yong Wei, Yu-Quan Molecules Article A novel series of 2-(3-fluoro-4-nitrophenoxy)-N-phenylacetamide compounds were designed, synthesized and in vitro assessed for their antitubercular activities by a microdilution method. All the novel derivatives exerted potent or moderate active against M. tuberculosis H(37)Rv, with MIC values ranging from 4 to 64 μg/mL. The most potent derivative 3m showed an identical MIC value of 4 μg/mL for both M. tuberculosis H(37)Rv and rifampin-resistant M. tuberculosis 261. It demonstrated no inhibitory effects against six different tumor cell lines by a MTT assay and had a good safety profile in a vero cell line, providing a good lead for subsequent optimization in search of novel affordable antitubercular agents. MDPI 2012-02-22 /pmc/articles/PMC6268079/ /pubmed/22357321 http://dx.doi.org/10.3390/molecules17022248 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Ang, Wei
Lin, Yan-Ni
Yang, Tao
Yang, Jian-Zhong
Pi, Wei-Yi
Yang, Ying-Hong
Luo, You-Fu
Deng, Yong
Wei, Yu-Quan
Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title_full Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title_fullStr Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title_full_unstemmed Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title_short Synthesis and Biological Evaluation of 2-(3-Fluoro-4-nitro phenoxy)-N-phenylacetamide Derivatives as Novel Potential Affordable Antitubercular Agents
title_sort synthesis and biological evaluation of 2-(3-fluoro-4-nitro phenoxy)-n-phenylacetamide derivatives as novel potential affordable antitubercular agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268079/
https://www.ncbi.nlm.nih.gov/pubmed/22357321
http://dx.doi.org/10.3390/molecules17022248
work_keys_str_mv AT angwei synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT linyanni synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT yangtao synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT yangjianzhong synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT piweiyi synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT yangyinghong synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT luoyoufu synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT dengyong synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents
AT weiyuquan synthesisandbiologicalevaluationof23fluoro4nitrophenoxynphenylacetamidederivativesasnovelpotentialaffordableantitubercularagents