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. 2014 Jan 15;19(1):925-39.
doi: 10.3390/molecules19010925.

Synthesis and broad-spectrum antiviral activity of some novel benzo-heterocyclic amine compounds

Da-Jun Zhang  1 , Wen-Fang Sun  1 , Zhao-Jin Zhong  1 , Rong-Mei Gao  1 , Hong Yi  1 , Yu-Huan Li  1 , Zong-Gen Peng  2 , Zhuo-Rong Li  3
Affiliations

Synthesis and broad-spectrum antiviral activity of some novel benzo-heterocyclic amine compounds

Da-Jun Zhang et al. Molecules. .

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.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
The chemical structure of the designed target compounds.
Scheme 1
Scheme 1
Synthetic route to the target compounds 1a–4b.
See this image and copyright information in PMC

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