摘要/Abstract

为了探寻新型的生物活性化合物，设计并合成了12个未见文献报道的新型哌啶噻唑类衍生物.生物活性测试研究发现，在500 μg/mL浓度下，目标化合物对粘虫表现出良好的抑制活性，而且在100 μg/mL下，（4-（5-（3-氯苯基）-4-甲基噻唑-2-基）哌啶-1-基）（4-甲基哌嗪-1-基）甲酮（1f）、（5-（3-氯苯基）-4-甲基噻唑-2-基）哌啶-1-基）（4-硝基-1H-吡唑-3-基）甲酮（1g）对粘虫的抑制率均达80%以上，另外在20 μg/mL下（5-（3-氯苯基）-4-甲基噻唑-2-基）哌啶-1-基）（4-硝基-1H-吡唑-3-基）甲酮（1g）仍具有50%的杀虫活性.
关键词: 氟噻唑吡乙酮, 哌啶噻唑类衍生物, 杀虫活性
Twelve new piperdine thiazole compounds were designed and synthesized in search of new bioactive compounds. The preliminary bioassay showed that at the concentration of 500 μg/mL the lethal rates of the target compounds possessed certain insceticidal activities against armyworm, and at the concentration of 100 μg/mL the lethal rates of (4-(5-(3-chloro-phenyl) -4-methylthiazol-2-yl) piperidin-1-yl) (4-methylpiperazin-1-yl) methanone (1f) and (4-(5-(4-chlorophenyl) -4-methyl-thiazol-2-yl) piperidin-1-yl) nitro-1H-pyrazol-3-yl) methanone (1g) against armyworm were 80% and 100%, respectively. Further screening at concentrations of 20 μg/mL, the lethal rate of (4-(5-(4-chlorophenyl) -4-methylthiazol-2-yl) piperidin-1-yl) (4-nitro-1H-pyrazol-3-yl) methanone (1g) against armyworm was 50%.
Key words: oxathiapiprolin, piperidine-thiazolederivatives, insecticidal activity


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