RESULTS: A laboratory colony of P. canaliculata was developed, which showed no difference in sensitivity to niclosamide compared with the wild group, while exhibiting a higher stability against pesticide response. Mitochondrial adenosine triphosphate (ATP) synthase inhibitors and mitochondrial membrane potential uncouplers were identified and validated as potential targets for molluscicide screening against P. canaliculata. A series of arylpyrrole compounds were designed and synthesized. The median lethal concentration of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile (Compound 102) was 10-fold lower than that of niclosamide.
CONCLUSIONS: New molluscicide targets were discovered and validated, and preliminary strategies were explored for pesticide screening based on these targets. Compound 102 exhibited a high molluscicidal activity and had a great potential value for exploring a molluscicide to control P. canaliculata. © 2024 Society of Chemical Industry.
结果:开发了泪珠菌的实验室菌落,与野生组相比,对氯硝柳胺的敏感性没有差异,同时对农药反应表现出更高的稳定性。线粒体三磷酸腺苷(ATP)合成酶抑制剂和线粒体膜电位解偶联剂被鉴定并验证为针对小泪虫的杀软体动物剂筛选的潜在靶标。设计并合成了一系列芳基吡咯化合物。4-溴-2-(4-氯苯基)-5-(三氟甲基)-1H-吡咯-3-甲腈(化合物102)的致死浓度中位数(LC50)比氯硝柳胺低10倍。
结论:发现并验证了新的杀软体动物靶标,并根据这些目标探索了农药筛选的初步策略。化合物102表现出较高的杀软体动物活性,并且对于探索一种杀软体动物剂以控制小泪虫具有很大的潜在价值。本文受版权保护。保留所有权利。