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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 *
Received: 28 November 2013; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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(1):925-939.

Chicago/Turabian Style

Zhang, Da-Jun; Sun, Wen-Fang; Zhong, Zhao-Jin; Gao, Rong-Mei; Yi, Hong; Li, Yu-Huan; Peng, Zong-Gen; Li, Zhuo-Rong. 2014. "Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds." Molecules 19, no. 1: 925-939.



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