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...
Autores principales: | , , , , , , , , |
---|---|
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 |