Design,Synthesis and Anti-Tobacco Mosaie Virus Activities of Echinopsine Derivatives Containing Acylhydrazone Indole Fragment
In order to discover highly active antiviral compounds,echinopsine was used as the lead and 15 echinopsine derivatives containing the acylhydrazone indole fragments were designed and synthesized by scaffold hopping strategy.Their structures were characterized using 1H NMR,13C NMR and HRMS.The in vivo antiviral activities against tobacco mosaic virus(TMV)were evaluated in three modes(inactivation,curative,and protective).Bioassay results revealed that some compounds exhibit high anti-TMV activities.The inactivation,curative and protective activites of compound 4n(43.5％,40.1％,38.7％)are superior to ribavirin and lead compound L2.The inactivation activities of compounds 4d(40.8％)and 4f(42.0％)are higher than that of ribavirin(38.6％)and lead compound L2(40.5％).The inactivation activity of compound 4I(38.4％)is equivalent to ribavirin(38.6％).The protective activity of compound 4f(36.4％)is equivalent to ribavirin(37.2％).Compound 4n is expected to become a potential antiviral pesticide.
NETL
NSTL
万方数据
