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Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds
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Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds
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Journal Article
Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds
2014
Overview
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.
Publisher
MDPI AG,MDPI
Subject
Antiviral Agents - chemical synthesis
/ Antiviral Agents - pharmacology
/ Benzimidazoles - chemical synthesis
/ Benzimidazoles - pharmacology
/ Benzothiazoles - chemical synthesis
/ Benzothiazoles - pharmacology
/ broad-spectrum antiviral activity
/ Hepatitis B virus - drug effects
/ Influenza A virus - drug effects
/ SAR
/ Structure-Activity Relationship
/ unsaturated five-membered benzo-heterocyclic amines
/ Vaccines
/ Viruses
