Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids

A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H(37)Rv (minim...

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Autores principales: Xu, Zhi, Zhang, Shu, Feng, Lian-Shun, Li, Xiao-Ning, Huang, Guo-Cheng, Chai, Yun, Lv, Zao-Sheng, Guo, Hui-Yuan, Liu, Ming-Liang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152256/
https://www.ncbi.nlm.nih.gov/pubmed/28703766
http://dx.doi.org/10.3390/molecules22071171
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author Xu, Zhi
Zhang, Shu
Feng, Lian-Shun
Li, Xiao-Ning
Huang, Guo-Cheng
Chai, Yun
Lv, Zao-Sheng
Guo, Hui-Yuan
Liu, Ming-Liang
author_facet Xu, Zhi
Zhang, Shu
Feng, Lian-Shun
Li, Xiao-Ning
Huang, Guo-Cheng
Chai, Yun
Lv, Zao-Sheng
Guo, Hui-Yuan
Liu, Ming-Liang
author_sort Xu, Zhi
collection PubMed
description A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H(37)Rv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06–4 μg/mL), and most Gram-negative strains (MIC: ≤0.03–4 μg/mL).
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spelling pubmed-61522562018-11-13 Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids Xu, Zhi Zhang, Shu Feng, Lian-Shun Li, Xiao-Ning Huang, Guo-Cheng Chai, Yun Lv, Zao-Sheng Guo, Hui-Yuan Liu, Ming-Liang Molecules Article A series of novel 8-OMe ciprofloxacin (CPFX)-hydrazone/azole hybrids were designed, synthesized, and evaluated for their in vitro biological activities. Our results reveal that all of the hydrozone-containing hybrids (except for 7) show potency against Mycobacterium tuberculosis (MTB) H(37)Rv (minimum inhibitory concentration (MIC): <0.5 μM), which is better than the parent drug CPFX, and comparable to moxifloxacin and isoniazid, some of the tested Gram-positive strains (MIC: 0.06–4 μg/mL), and most Gram-negative strains (MIC: ≤0.03–4 μg/mL). MDPI 2017-07-13 /pmc/articles/PMC6152256/ /pubmed/28703766 http://dx.doi.org/10.3390/molecules22071171 Text en © 2017 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
Xu, Zhi
Zhang, Shu
Feng, Lian-Shun
Li, Xiao-Ning
Huang, Guo-Cheng
Chai, Yun
Lv, Zao-Sheng
Guo, Hui-Yuan
Liu, Ming-Liang
Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title_full Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title_fullStr Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title_full_unstemmed Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title_short Synthesis and In Vitro Antimycobacterial and Antibacterial Activity of 8-OMe Ciprofloxacin-Hydrozone/Azole Hybrids
title_sort synthesis and in vitro antimycobacterial and antibacterial activity of 8-ome ciprofloxacin-hydrozone/azole hybrids
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152256/
https://www.ncbi.nlm.nih.gov/pubmed/28703766
http://dx.doi.org/10.3390/molecules22071171
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