The discovery of indazapyroxamet: a novel 3-pyridinyl insecticide targeting piercing/sucking insectsa .
Wenming Zhang, Rachel D Slack, Michael A Rossi, Jason Hamm, Daniel Cordova, David Clark, George Lahm, Moumita Kar, Kashinath Sana, Ming Xu, Andrew DeAngelis, Breena Fraga
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Abstract
In recent years, the registrations for a number of commercial insecticides utilized for piercing/sucking insects have been cancelled or restricted. To meet this growing need for new hemipteran controlling agrochemicals, we discovered a 2-(pyridin-3-yl)-thiazole compound, with limited insecticidal activity against cotton/melon aphid (Aphis gossypii). The 2-(pyridin-3-yl)-thiazole moiety offered us a basis to pursue the bicyclic 2-(pyridin-3-yl)-2H-indazole carboxamides. Evaluation of such 2-(pyridin-3-yl)-2H-indazole carboxamides revealed that even analogs containing only simple alkyl amides attached at the 4 or 5 positions possess promising insecticidal activity. Extensive optimization of this novel class of 2-(pyridin-3-yl)-2H-indazole carboxamides led to identifying indazapyroxamet for commercial development. © 2024 Society of Chemical Industry.
发现茚虫威:一种针对穿刺/吸食昆虫的新型 3-吡啶基杀虫剂a。
近年来,一些用于刺吸式昆虫的商业杀虫剂的登记已被取消或受到限制。为了满足对新型半翅目昆虫防治农用化学品日益增长的需求,我们发现了一种 2-(吡啶-3-基)噻唑化合物,它对棉花/西瓜蚜虫(Aphis gossypii)具有有限的杀虫活性。2-(吡啶-3-基)-噻唑分子为我们开发双环 2-(吡啶-3-基)-2H-吲唑羧酰胺提供了基础。对此类 2-(吡啶-3-基)-2H-吲唑羧酰胺的评估表明,即使是仅在 4 或 5 位上连接简单烷基酰胺的类似物,也具有良好的杀虫活性。通过对这一类新型 2-(吡啶-3-基)-2H-吲唑羧酰胺进行广泛优化,最终确定了可用于商业开发的茚虫威。© 2024 化学工业协会。
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