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

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. Nota...

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Detalles Bibliográficos
Autores principales: Zhang, Da-Jun, Sun, Wen-Fang, Zhong, Zhao-Jin, Gao, Rong-Mei, Yi, Hong, Li, Yu-Huan, Peng, Zong-Gen, Li, Zhuo-Rong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271935/
https://www.ncbi.nlm.nih.gov/pubmed/24434668
http://dx.doi.org/10.3390/molecules19010925
Descripción
Sumario: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 (IC(50) = 3.21–5.06 μM) and 3g (IC(50) = 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.