Acetylcholinesterase cysteine-targeted insecticides against malaria vector Anopheles gambia and other mosquitos have already been introduced. We have applied the olefin metathesis for the preparation of cysteine-targeted insecticides in high yields. The prepared compounds with either a succinimide or maleimide moiety were evaluated on Anopheles gambiae and human acetylcholinesterase with relatively high irreversible inhibition of both enzymes but poor selectivity. The concept of cysteine binding was not proved by several methods, and poor stability was observed of the chosen most potent/selective compounds in a water/buffer environment. Thus, our findings do not support the proposed concept of cysteine-targeted selective insecticides for the prepared series of succinimide or maleimide compounds.

中文翻译：

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针对冈比亚曲霉乙酰胆碱酯酶的半胱氨酸靶向杀虫剂既不是选择性抑制剂也不是可逆抑制剂。

针对疟疾媒介冈比亚按蚊和其他蚊子的针对乙酰胆碱酯酶半胱氨酸的杀虫剂已经被引入。我们已经将烯烃复分解用于制备高产率的以半胱氨酸为目标的杀虫剂。在冈比亚按蚊和人乙酰胆碱酯酶上对制备的具有琥珀酰亚胺或马来酰亚胺部分的化合物进行了评估，两种酶均具有较高的不可逆抑制性，但选择性较差。半胱氨酸结合的概念没有通过几种方法得到证实，并且在水/缓冲液环境中观察到所选最有效/选择性化合物的稳定性差。因此，我们的发现不支持所制备的一系列琥珀酰亚胺或马来酰亚胺化合物的半胱氨酸靶向选择性杀虫剂的概念。