Design,Synthesis and Biological Evaluation of Novel N-(4-([2,2':5',2''-Terthiophen]-5-yl)-2-methylbut-3-yn-2-yl)Benzamide Derivatives

On the basis of the principle of combination of active groups,a series of novel N-(4-([2,2':5',2''-terthiophen]-5-yl)-2-methylbut-3-yn-2-yl)benzamide derivatives were designed,synthesized and systematically evaluated for their antiviral activity against tobacco mosaic virus(TMV).The bioassay results showed that most of these compounds displayed good anti-TMV activity,and some of them exhibited higher antiviral activity than commercial Ningnanmycin.Especially,compound 8e with excellent anti-TMV activity(inactivation activity,92.3%/500μg•mL^(−1);curative activity,85.7%/500μg•mL^(−1) and protection activity,64.7%/500μg•mL^(−1))emerged as a potential inhibitor of plant virus TMV.Quantitative structure-activity relationship studies proved that the van der Waals volume(V)and electronic parameter(Σ(Σσo+σp)andΣσm)for the substituent R1 were very important for antiviral activities in this class of compounds.