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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...

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Detalles Bibliográficos
Autores principales: Zhang, Da-Jun, Sun, Wen-Fang, Zhong, Zhao-Jin, Gao, Rong-Mei, Yi, Hong, Li, Yu-Huan, Peng, Zong-Gen, Li, Zhuo-Rong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
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.
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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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