Antiviral properties and interaction of novel chalcone derivatives containing a purine and benzenesulfonamide moiety

作者：Zhou, Dagui; Xie, Dandan; He, Fangcheng; Song, Baoan; Hu, Deyu^*

来源：Bioorganic & Medicinal Chemistry Letters, 2018, 28(11): 2091-2097.

DOI：10.1016/j.bmcl.2018.04.042

• Chalcone derivatives
• Purine moiety
• Benzenesulfonamide moiety
• Antiviral property
• Tobacco mosaic virus
• Cucumber mosaic virus

A new concise and facile method was explored to synthesize a series of novel chalcone derivatives containing a purine and benzenesulfonamide moiety and their antiviral properties were evaluated against TMV and CMV. Biological assays indicated that several of the derivatives exhibited significant anti-TMV and anti-CMV activities in vivo. In particular, compound d2 displayed excellent inactivating activity against TMV, with the EC50 value of 51.65 mu g/mL, which was better than that of ribavirin (150.45 mu g/mL). Molecular docking showed that there are four hydrogen bonds between compound d2 and TMV coat protein (TMV-CP). Compound d2 demonstrated strong binding capacity to TMV-CP with K-a = 1.58 x 10(5) L/mol and K-d = 12.16 mu M. These findings indicated that chalcone derivatives are worthy of further research and development as templates for new antiviral agents.

• 出版日期2018-6-15
• 单位贵州大学