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Design, Synthesis And Biological Evaluation Of Novel N-(4-([2,2′:5′,2′′-Terthiophen]-5-yl)-2-methylbut-3-yn-2-yl) Benzamide Derivatives
Published 2015 · Chemistry
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%/500 µg·mL−1; curative activity, 85.7%/500 µg·mL−1 and protection activity, 64.7%/500 µg·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 (∑(∑σo+σp) and ∑σm) for the substituent R1 were very important for antiviral activities in this class of compounds.