Design,synthesis and anti-TMV activity of novel quinolinone derivatives
[Aims]This study aims to develop green and efficient viral inhibitors by structural modification of natural product.[Methods]Using echinopsine as lead compound,1-(2-hydroxy-ethyl)-1H-quinolin-4-one(intermediate 1)and 24 novel quinolinone derivatives with ester groups at position 1 were designed and synthesized by introduction of active functional groups.The in vivo anti-tobacco mosaic virus(anti-TMV)activities were evaluated in inactivation,curative,and protection modes.[Results]Their structures were confirmed by HRMS,1H NMR and 13C NMR.Eight compounds showed higher anti-TMV activities than ribavirin,among which intermediate 1(44.2％,57.3％,50.4％),3a(47.3％,41.0％,42.3％)and 3d(45.8％,44.9％,47.2％)showed the highest inactivation,curative and protection activities against TMV.[Conclusions]Intermediate 1,compounds 3a and 3d can be used as antiviral lead compounds for further structural optimization.
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