Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy

A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625–6.25 μg/mL...

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Autores principales: Cheng, Ya-Juan, Liu, Zhi-Yong, Liang, Hua-Ju, Fang, Cui-Ting, Zhang, Niu-Niu, Zhang, Tian-Yu, Yan, Ming
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6572244/
https://www.ncbi.nlm.nih.gov/pubmed/31137832
http://dx.doi.org/10.3390/molecules24102021
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author Cheng, Ya-Juan
Liu, Zhi-Yong
Liang, Hua-Ju
Fang, Cui-Ting
Zhang, Niu-Niu
Zhang, Tian-Yu
Yan, Ming
author_facet Cheng, Ya-Juan
Liu, Zhi-Yong
Liang, Hua-Ju
Fang, Cui-Ting
Zhang, Niu-Niu
Zhang, Tian-Yu
Yan, Ming
author_sort Cheng, Ya-Juan
collection PubMed
description A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625–6.25 μg/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against cell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection model via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class of new antitubercular agents with good potential.
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spelling pubmed-65722442019-06-18 Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy Cheng, Ya-Juan Liu, Zhi-Yong Liang, Hua-Ju Fang, Cui-Ting Zhang, Niu-Niu Zhang, Tian-Yu Yan, Ming Molecules Article A series of 3-amino-5-benzylphenol derivatives were designed and synthesized. Among them, (3-benzyl-5-hydroxyphenyl)carbamates were found to exert good inhibitory activity against M. tuberculosis H37Ra, H37Rv and clinically isolated multidrug-resistant M. tuberculosis strains (MIC = 0.625–6.25 μg/mL). The privileged compounds 3i and 3l showed moderate cytotoxicity against cell line A549. Compound 3l also exhibited potent in vivo inhibitory activity on a mouse infection model via the oral administration. The results demonstrated 3-hydroxyphenylcarbamates as a class of new antitubercular agents with good potential. MDPI 2019-05-27 /pmc/articles/PMC6572244/ /pubmed/31137832 http://dx.doi.org/10.3390/molecules24102021 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Cheng, Ya-Juan
Liu, Zhi-Yong
Liang, Hua-Ju
Fang, Cui-Ting
Zhang, Niu-Niu
Zhang, Tian-Yu
Yan, Ming
Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title_full Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title_fullStr Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title_full_unstemmed Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title_short Discovery of (3-Benzyl-5-hydroxyphenyl)carbamates as New Antitubercular Agents with Potent In Vitro and In Vivo Efficacy
title_sort discovery of (3-benzyl-5-hydroxyphenyl)carbamates as new antitubercular agents with potent in vitro and in vivo efficacy
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6572244/
https://www.ncbi.nlm.nih.gov/pubmed/31137832
http://dx.doi.org/10.3390/molecules24102021
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