Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors

European Journal of Medicinal Chemistry
2012.0

Abstract

The influenza virus is a persistent cause of mortality and morbidity on an annual basis and thus presents itself as an important target for pharmaceutical investigation. In this work, substituted bisaryl amide compounds were found to be a new class of potential anti-influenza agents, and a series of substituted bisaryl amide compounds were synthesised and evaluated for their anti-influenza virus activities. The analysis of the results produced a preliminary structure-activity relationship study (SAR). Compounds 1a, 1g, 1h, 1j, 1l and 1n exhibited clear antiviral activities against the influenza A (A/Guangdong Luohu/219/2006, H1N1) virus with 50% inhibitory concentrations (IC(50)) for virus growth ranging from 12.5 to 59.0 μM. Specifically, compound 1j also possessed antiviral activity against both oseltamivir-resistant influenza (A/Jinnan/15/2009) virus and influenza B (B/Jifang/13/97) virus with IC(50) values of 9.2 μM and 21.4 μM, respectively. Compound 1j is thus worth further investigation as an anti-influenza virus candidate.

Knowledge Graph

Similar Paper

Synthesis and antiviral activity of substituted bisaryl amide compounds as novel influenza virus inhibitors
European Journal of Medicinal Chemistry 2012.0
Synthesis and biological evaluation of novel bisheterocycle-containing compounds as potential anti-influenza virus agents
Bioorganic & Medicinal Chemistry Letters 2005.0
1,6-Bis[(benzyloxy)methyl]uracil derivatives—Novel antivirals with activity against HIV-1 and influenza H1N1 virus
Bioorganic & Medicinal Chemistry 2016.0
Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents
Bioorganic & Medicinal Chemistry Letters 2019.0
New type of anti-influenza agents based on benzo[d][1,3]dithiol core
Bioorganic & Medicinal Chemistry Letters 2020.0
Design and synthesis of heteroaromatic-based benzenesulfonamide derivatives as potent inhibitors of H5N1 influenza A virus
MedChemComm 2018.0
Design, synthesis and anti-influenza A virus activity of novel 2,4-disubstituted quinazoline derivatives
Bioorganic & Medicinal Chemistry Letters 2020.0
Synthesis and Antiviral Activity Evaluation of Some New Aminoadamantane Derivatives. 2
Journal of Medicinal Chemistry 1996.0
Design, synthesis and in vitro anti-influenza A virus evaluation of novel quinazoline derivatives containing S-acetamide and NH-acetamide moieties at C-4
European Journal of Medicinal Chemistry 2020.0
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives
Bioorganic & Medicinal Chemistry 2012.0