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Molecules 2014, 19(1), 925-939; doi:10.3390/molecules19010925
Article

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

, , , , , , *  and *
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 28 November 2013 / Revised: 8 January 2014 / Accepted: 9 January 2014 / Published: 15 January 2014
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: unsaturated five-membered benzo-heterocyclic amines; broad-spectrum antiviral activity; DNA and RNA virus; SAR unsaturated five-membered benzo-heterocyclic amines; broad-spectrum antiviral activity; DNA and RNA virus; SAR
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Zhang, D.-J.; Sun, W.-F.; Zhong, Z.-J.; Gao, R.-M.; Yi, H.; Li, Y.-H.; Peng, Z.-G.; Li, Z.-R. Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds. Molecules 2014, 19, 925-939.

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