杀虫氨基甲酸酯类的构效关系
Structure-activity relationships for insecticidal carbamates.
作者信息
Metcalf R L
出版信息
Bull World Health Organ. 1971;44(1-3):43-78.
Abstract
Carbamate insecticides are biologically active because of their structural complementarity to the active site of acetylcholinesterase (AChE) and their consequent action as substrates with very low turnover numbers. Carbamates behave as synthetic neurohormones that produce their toxic action by interrupting the normal action of AChE so that acetylcholine accumulates at synaptic junctions. The necessary properties for a suitable insecticidal carbamate are lipid solubility, suitable structural complementarity to AChE, and sufficient stability to multifunction-oxidase detoxification. The relationships between the structure and the activity of a large number of synthetic carbamates are analysed in detail, with particular attention to the second of these properties.
摘要
氨基甲酸酯类杀虫剂具有生物活性，因为它们在结构上与乙酰胆碱酯酶（AChE）的活性位点互补，从而作为周转数极低的底物发挥作用。氨基甲酸酯类作为合成神经激素，通过中断AChE的正常作用产生毒性作用，使乙酰胆碱在突触连接处积累。一种合适的杀虫氨基甲酸酯所需的特性是脂溶性、与AChE合适的结构互补性以及对多功能氧化酶解毒作用有足够的稳定性。详细分析了大量合成氨基甲酸酯的结构与活性之间的关系，尤其关注这些特性中的第二个特性。
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