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N-取代马来酰胺酯衍生的新型二硫代磷酸酯的合成与生物活性

Synthesis and bioactivity of new phosphorodithioates derived from N-substituted maleamic esters.

作者信息

de Licastro S A, Wallace G, Seccacini E, Gonzalez Audino P, Zerba E

机构信息

Centro de Investigaciones de plagas e insecticidas CIPEIN (CITEFA-CONICET), Buenos Aires, Argentina.

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1993 Jan;104(1):43-6. doi: 10.1016/0742-8413(93)90108-w.

Abstract
  1. A new series of organophosphorus compounds derived from N-substituted maleamic esters by reaction with dimethyl and diethyl phosphorodithioic acid was synthesized. 2. Two isomers, with chemical structures analogous to malathion were obtained for each maleamic ester assayed. 3. They were characterized, and their toxicity against a resistant strain of Musca domestica (strain G), a susceptible one (strain RAC) and Triatoma infestans (vector of Chagas' disease) were measured. 4. The structural chemical modification introduced by replacing a carboxyester group for a N-substituted amido one, reverted the resistance obtained for malathion. 5. Replacement of methyl by ethyl dithiophosphoric acid did not introduce significative differences. 6. In the case of Triatoma infestans, the synthesized compounds were less active than malathion.
摘要
  1. 通过N-取代马来酰胺酯与二甲基和二乙基二硫代磷酸反应合成了一系列新的有机磷化合物。2. 对每种测定的马来酰胺酯,都得到了两种化学结构类似于马拉硫磷的异构体。3. 对它们进行了表征,并测定了它们对家蝇抗性品系(G品系)、敏感品系(RAC品系)和克氏锥虫病传播媒介骚扰锥蝽的毒性。4. 用N-取代酰胺基取代羧基酯基团所引入的结构化学修饰,逆转了马拉硫磷所产生的抗性。5. 用乙二硫代磷酸取代甲二硫代磷酸未产生显著差异。6. 对于骚扰锥蝽,合成的化合物活性低于马拉硫磷。

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