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Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds

Authors :
Wen-Fang Sun
Yu-Huan Li
Rong-Mei Gao
Dajun Zhang
Hong Yi
Zhuorong Li
Zhao-Jin Zhong
Zong-Gen Peng
Source :
Molecules, Vol 19, Iss 1, Pp 925-939 (2014), Molecules, Molecules; Volume 19; Issue 1; Pages: 925-939
Publication Year :
2014
Publisher :
MDPI AG, 2014.

Abstract

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 (IC50 = 3.21–5.06 μM) and 3g (IC50 = 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.

Details

Language :
English
ISSN :
14203049
Volume :
19
Issue :
1
Database :
OpenAIRE
Journal :
Molecules
Accession number :
edsair.doi.dedup.....3487a6a27e72cda2fbef2a6bd6fb4184