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.
Highlights
Viral infections pose a threat to virtually every organism in every domain of life
The chemical structures of the synthesized target compounds were all confirmed by 1H-NMR, 13C-NMR and HRMS
The synthesized target compounds were assayed for their broad spectrum antiviral activity towards influenza A, Hepatitis B virus (HBV), hepatitis C virus (HCV) and Cox B3 virus in vitro
Summary
Viral infections pose a threat to virtually every organism in every domain of life. People over 65 years of age account for 90% of seasonal influenza-associated deaths, and influenza viruses with either high mortality or morbidity have heightened fears that the influenza pandemic will occur. A vaccine has been developed, chronic hepatitis B (CHB) caused by hepatitis virus infection is still one of the most serious human viral infectious diseases worldwide. We have reported a novel class of (5-oxazolyl)phenyl amines that act as potential inosine monophosphate dehydrogenase (IMPDH) inhibitors and exhibit broad-spectrum antiviral activities [14]. In continuance of our endeavor to search for novel antiviral agents with broad-spectrum antiviral activity, we designed a novel class of unsaturated five-membered benzo-heterocyclic derivatives using a ring transforming strategy that is based on our previously reported structures (Figure 1). A novel class of unsaturated five-membered benzo-heterocyclesubstituted amines were synthesized and assayed for their broad spectrum antiviral activity in vitro, and their structure-activity relationships (SARs) were investigated. Reagents and conditions: (a) 10% Pd/C, H2(50 psi), EtOH, rt; and (b) various substituted aldehydes, EtOH, rt or reflux, 8 h, NaBH4, rt, 3 h
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