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

作　　者：Youquan Zhu Haili Zhang Danyang Wang Lei Li Han Xu Huabin Li Yuan Ma 

机构地区：[1]State Key Laboratory of Elemento-Organic Chemistry,Institute of Elemento-Organic Chemistry,Collaborative Innovation Center of Chemical Science and Engineering(Tianjin),Nankai University,Tianjin 300071,China

出　　处：《Chinese Journal of Chemistry》2015年第2期268-276,共9页中国化学（英文版）

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).

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.

关 键 词：α-terthienyl BENZAMIDE antiviral activity tobacco mosaic virus tobacco mosaic virus(TMV) 

分 类 号：O62[理学—有机化学]