摘要
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.
基金
support by the National Basic Research Program of China(973 Program)(No.2010CB126103)
the National Natural Science Foundation of China(Nos.21372134,21072108,21102078)
NFFTBS(No.J1103306)
the National Key Technologies R&D Program(No.2011BAE06B05-3)
Collaborative Innovation Center of Chemical Science and Engineering(Tianjin).
