Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives

A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro...

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Autores principales: Bao, Beihua, Meng, Zheng, Li, Nianguang, Meng, Zhengjie, Zhang, Li, Cao, Yudan, Yao, Weifeng, Shan, Mingqiu, Ding, Anwei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3759959/
https://www.ncbi.nlm.nih.gov/pubmed/23965980
http://dx.doi.org/10.3390/ijms140817193
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author Bao, Beihua
Meng, Zheng
Li, Nianguang
Meng, Zhengjie
Zhang, Li
Cao, Yudan
Yao, Weifeng
Shan, Mingqiu
Ding, Anwei
author_facet Bao, Beihua
Meng, Zheng
Li, Nianguang
Meng, Zhengjie
Zhang, Li
Cao, Yudan
Yao, Weifeng
Shan, Mingqiu
Ding, Anwei
author_sort Bao, Beihua
collection PubMed
description A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC(50) values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC(50) values being 96.4, 71.0 and 75.4 μM, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin.
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spelling pubmed-37599592013-09-03 Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives Bao, Beihua Meng, Zheng Li, Nianguang Meng, Zhengjie Zhang, Li Cao, Yudan Yao, Weifeng Shan, Mingqiu Ding, Anwei Int J Mol Sci Article A series of schizonepetin derivatives have been designed and synthesized in order to obtain potent antivirus agents. The antiviral activity against HSV-1 and influenza virus H3N2 as well as the cytotoxicity of these derivatives was evaluated by using cytopathic effect (CPE) inhibition assay in vitro. Compounds M2, M4, M5 and M34 showed higher inhibitory activity against HSV-1 virus with the TC(50) values being in micromole. Compounds M28, M33, and M35 showed higher inhibitory activity against influenza virus H3N2 with their TC(50) values being 96.4, 71.0 and 75.4 μM, respectively. Preliminary biological activity evaluation indicated that the anti-H3N2 and anti-HSV-1 activities improved obviously through the introduction of halogen into the structure of schizonepetin. Molecular Diversity Preservation International (MDPI) 2013-08-20 /pmc/articles/PMC3759959/ /pubmed/23965980 http://dx.doi.org/10.3390/ijms140817193 Text en © 2013 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
Bao, Beihua
Meng, Zheng
Li, Nianguang
Meng, Zhengjie
Zhang, Li
Cao, Yudan
Yao, Weifeng
Shan, Mingqiu
Ding, Anwei
Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title_full Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title_fullStr Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title_full_unstemmed Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title_short Design, Synthesis and Antiviral Activity Studies of Schizonepetin Derivatives
title_sort design, synthesis and antiviral activity studies of schizonepetin derivatives
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3759959/
https://www.ncbi.nlm.nih.gov/pubmed/23965980
http://dx.doi.org/10.3390/ijms140817193
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