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Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds
A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Nota...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271935/ https://www.ncbi.nlm.nih.gov/pubmed/24434668 http://dx.doi.org/10.3390/molecules19010925 |
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author | Zhang, Da-Jun Sun, Wen-Fang Zhong, Zhao-Jin Gao, Rong-Mei Yi, Hong Li, Yu-Huan Peng, Zong-Gen Li, Zhuo-Rong |
author_facet | Zhang, Da-Jun Sun, Wen-Fang Zhong, Zhao-Jin Gao, Rong-Mei Yi, Hong Li, Yu-Huan Peng, Zong-Gen Li, Zhuo-Rong |
author_sort | Zhang, Da-Jun |
collection | PubMed |
description | A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC(50) = 3.21–5.06 μM) and 3g (IC(50) = 0.71–34.87 μM) showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus) and a DNA virus (HBV) at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses. |
format | Online Article Text |
id | pubmed-6271935 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62719352018-12-20 Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds Zhang, Da-Jun Sun, Wen-Fang Zhong, Zhao-Jin Gao, Rong-Mei Yi, Hong Li, Yu-Huan Peng, Zong-Gen Li, Zhuo-Rong Molecules Article A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC(50) = 3.21–5.06 μM) and 3g (IC(50) = 0.71–34.87 μM) showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus) and a DNA virus (HBV) at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses. MDPI 2014-01-15 /pmc/articles/PMC6271935/ /pubmed/24434668 http://dx.doi.org/10.3390/molecules19010925 Text en © 2014 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 license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Zhang, Da-Jun Sun, Wen-Fang Zhong, Zhao-Jin Gao, Rong-Mei Yi, Hong Li, Yu-Huan Peng, Zong-Gen Li, Zhuo-Rong Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title | Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title_full | Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title_fullStr | Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title_full_unstemmed | Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title_short | Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds |
title_sort | synthesis and broad-spectrum antiviral activity of some novel benzo-heterocyclic amine compounds |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271935/ https://www.ncbi.nlm.nih.gov/pubmed/24434668 http://dx.doi.org/10.3390/molecules19010925 |
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