4.3 Article

Design, synthesis, and anti-tobacco mosaic virus activity evaluation of quinazolinone derivatives containing purine moieties

Journal

PHYTOCHEMISTRY LETTERS
Volume 59, Issue -, Pages 10-14

Publisher

ELSEVIER
DOI: 10.1016/j.phytol.2023.11.003

Keywords

Synthesis; Quinazolinone derivatives; Purine moiety; Tobacco mosaic virus; Antiviral activity; SAR analysis

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This study successfully designed and synthesized a series of quinazolinone derivatives containing purine molecules, and found that some compounds exhibited strong antiviral activity against tobacco mosaic virus. The findings have important implications for further development of antiviral drugs.
In this study, a series of quinazolinone derivatives containing purine molecules were designed and synthesized, and their structures were characterized by 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, and HRMS (High Resolution Mass Spectrometer). Antiviral bioassays against plant viruses indicated that some target compounds exhibited higher in vivo antiviral activity against tobacco mosaic virus (TMV) than the commercial drug ribavirin. At a concentration of 500 mg/L, compound A2 exhibited good activity against TMV, with therapeutic and protective activity values of 65.2 % and 60.2 %, respectively, and these values were superior to those of ribavirin (50.1 % and 57.2 %, respectively). Among these compounds, A2 demonstrated significant therapeutic bioactivity against TMV in vivo, with an EC50 (half-maximum effective concentration) value of 162.3 mg/L, which was superior to that of ribavirin (314.4 mg/L). In conclusion, quinazolinone derivatives containing purine molecules may provide a basis for further research on antiviral drugs.

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