Design,synthesis and bioactivities of novel bicyclic pyrazole carboxamide derivatives

来源 :第五届农药与环境安全国际学术研讨会暨第四届植保机械与施药技术国际研讨会( 5th International Sympo | 被引量 : 0次 | 上传用户:lialiaoliao
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  To discover novel pyrazole lead compounds with insecticidal activity,two series of novel carboxamide analogues(7a-v)containing N-substituted alkylbicyclic cycloheptapyrazole compounds were designed and synthesized.The target compounds were synthesized in four steps by diethyloxalate,cyclic ketone,sodium,etc.22 compounds were synthesized and their chemical structures were confirmed by 1H NMR,13C NMR,and high resolution mass spectroscopy(HRMS),and IR.The preliminary insecticidal activities results indicated that seven target compounds showed 100%mortality against Plutella xylostella.Those Plutella xylostella treated by target compounds showed the same poisoning symptoms as that of tebufenozide-treated.The preliminary structure-activity relationship analysis revealed that R group had regular pattern to pyrazole amide compounds.And it is helpful to enhance the biological activity of these compounds by reducing the number of branches of α-carbon or introducing cyclopropyl.In addition,cycloheptapyrazole 5-carboxylamides derivatives showed better activity than cycloheptapyrazole 3-carboxylamides derivatives.
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