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2 results on '"unsaturated five-membered benzo-heterocyclic amines"'

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

Author

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

Subjects
unsaturated five-membered benzo-heterocyclic amines, broad-spectrum antiviral activity, DNA and RNA virus, SAR, Organic chemistry, QD241-441
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.

Published
2014
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2. Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds

Author

Wen-Fang Sun, Yu-Huan Li, Rong-Mei Gao, Dajun Zhang, Hong Yi, Zhuorong Li, Zhao-Jin Zhong, and Zong-Gen Peng

Subjects
Hepatitis B virus, Stereochemistry, broad-spectrum antiviral activity, Pharmaceutical Science, Hepacivirus, Antiviral Agents, Virus, Article, Analytical Chemistry, lcsh:QD241-441, unsaturated five-membered benzo-heterocyclic amines, DNA and RNA virus, SAR, Broad spectrum, Structure-Activity Relationship, lcsh:Organic chemistry, Drug Discovery, Benzothiazoles, Physical and Theoretical Chemistry, IC50, Amine derivatives, chemistry.chemical_classification, Chemistry, Organic Chemistry, RNA, Influenza a, In vitro, Chemistry (miscellaneous), Influenza A virus, Heterocyclic amine, Molecular Medicine, Benzimidazoles
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.

Published
2014

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