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
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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.
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.
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.