Design,synthesis and anti-TMV activities of echinopsine derivatives containing 1,3,4-oxadiazole fragment
[Aims]This study aims to discover novel compounds with high anti-TMV activity.[Methods]The fragment of 1,3,4-oxadiazole was introduced into echinopsine through 4 steps including substitution,hydrazine hydrolysis,cyclization and substitution to synthesize 11 echinopsine derivatives containing 1,3,4-oxadiazole,and their anti-TMV activity were tested.[Results]The structures of the target compounds were confirmed by 1H NMR,13C NMR and HRMS.The activity test results showed that the anti-TMV activities of 8 echinopsine 1,3,4-oxadiazole derivatives were higher than that of ribavirin at 500 mg/L,with compounds 5d and 5j having the highest activity.[Conclusions]Compounds 5d and 5j can be used as lead compounds for further structural optimization.
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维普
