选择性有机磷杀虫剂的研究 阿赛硫磷(Acethion)类化合物的化学结构和生物活性

STUDIES ON SELECTIVE ORGANOPHOSPHORUS INSECTICIDES:CHEMICAL STRUCTURE AND BIOLOGICAL ACTIVITY OF ACETHION ANALOGS

本文研究了一系列阿赛硫磷(Acethion)类化合物对家蝇头部胆碱酯酶的抑制作用、被鼠肝羧酸酯酶的水解作用以及对家蝇(Musca domestica vicina Macq.)和小白鼠的毒性。化合物的羧酸酯酶水解速度(CO_2微升)的对数值和抗胆碱酯酶活性的负对数(pI_(50))与烷基诱导效应指数(I)之间都存在直线关系。化合物对家蝇毒性(LD_(50))的对数值与抗胆碱酯酶活性的负对数(pI_(50))之间大致有直线关系,但有些化合物距离直线较远,这可能由于在体内易于进行活化作用使毒性增高。化合物对小白鼠毒性(LD_(50))的对数值与羧酸酯酶水解速度(CO_2微升)对数值之间,没有直线关系。说明羧酸酯酶的水解作用不是此类化合物解毒作用的唯一因素,可能包括磷酸酶的水解作用。所合成的化合物大部分部有选择毒性,其中AP_d的选择比率(LD_(50))小白鼠/LD_(50)家蝇)最高,为221。

A series of O,O-dialkyl S-carboalkoxyalkyl phosphorodithioates were examined forhydrolysis rates by mouse liver enzyme, anticholinesterase activities to house fly cholines-terase and toxicities to house flies (Musca domestica vicina Macq.) and mice. Linear re-lationships between the logarithm of hydrolysis rate, and also pI_(50), and inductive effectindex (I) of the alkyl radical in the carboalkoxy group were observed. A rough linearrelationship between log LD_(50) (house fly) and pI_(50) was also observed with some devia-tions which are presumably due to the fact that several compounds are more easily ac-tivated in vivo. There is no correlation between mouse liver hydrolysis rate and toxicityto mice, and the evidence indicates that carboxyesterase hydrolysis is not the only factorof the detoxification of these compounds, in which phosphotase hydrolysis may be in-volved. Most of compounds listed in table 3 showed selective toxicity. Among these,AP_4 is the best with a selective ratio (LD_(50) mouse/LD_(50) house fly) of 221.