Journal
MOLECULES
Volume 19, Issue 1, Pages 925-939Publisher
MDPI
DOI: 10.3390/molecules19010925
Keywords
unsaturated five-membered benzo-heterocyclic amines; broad-spectrum antiviral activity; DNA and RNA virus; SAR
Funding
- National Natural Science Foundation of China [81273439]
- National Mega-project for Innovative Drugs [2012ZX09301002-001-024-02]
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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 mu M) and 3g (IC50 = 0.71-34.87 mu 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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