Molecules p. 925 - 939 (2014)
Update date:2022-08-02
Topics: Synthesis Chemical Synthesis Antiviral Activity Heterocyclic Chemistry Antiviral assay Broad-spectrum Benzo-heterocyclic amine compounds Bioactivity screening
Zhang, Da-Jun
Sun, Wen-Fang
Zhong, Zhao-Jin
Gao, Rong-Mei
Yi, Hong
Li, Yu-Huan
Peng, Zong-Gen
Li, Zhuo-Rong
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 M) and 3g (IC50 = 0.71-34.87 M) 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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