Molecules (Jan 2014)

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

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

DOI
https://doi.org/10.3390/molecules19010925
Journal volume & issue
Vol. 19, no. 1
pp. 925 – 939

Abstract

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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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