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 systemati...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.展开更多
A mild and efficient synthesis for the biaryl acids via rhodium-catalyzed cross-dehydrogenative coupling reaction has been developed. This novel protocol with sodium chlorite as an oxidant featured many advantages suc...A mild and efficient synthesis for the biaryl acids via rhodium-catalyzed cross-dehydrogenative coupling reaction has been developed. This novel protocol with sodium chlorite as an oxidant featured many advantages such as mild reaction conditions, high regioselectivity, tolerance of various functional groups, and good to excellent yields.展开更多
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)+2 种基金NFFTBS(No.J1103306)the National Key Technologies R&D Program(No.2011BAE06B05-3)Collaborative Innovation Center of Chemical Science and Engineering(Tianjin).
文摘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.
文摘A mild and efficient synthesis for the biaryl acids via rhodium-catalyzed cross-dehydrogenative coupling reaction has been developed. This novel protocol with sodium chlorite as an oxidant featured many advantages such as mild reaction conditions, high regioselectivity, tolerance of various functional groups, and good to excellent yields.
