Zhong Liangkun, Wu Changyuan, Li Mimi, Wu Junhui, Chen Yang, Ju Zhiran, Tan Chengxia
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
Institute of Pharmaceutical Science and Technology, Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China.
Org Biomol Chem. 2023 Sep 27;21(37):7511-7524. doi: 10.1039/d3ob00934c.
N,O-containing heterocycles have been incorporated into various approved pesticides and pesticide candidates. The persistent challenge in contemporary crop protection lies in the continuous pursuit of novel N,O-heterocycle-containing compounds with pesticidal properties. Among them, the 1,2,4-oxadiazole scaffold is one of the most extensively explored heterocycles in new pesticide discovery and development. This review focuses on elucidating the molecular design strategy employed along with highlighting the bioactivity of 1,2,4-oxadiazole derivatives since 2012. Throughout this time frame, tioxazafen and flufenoxadiazam have emerged as prominent examples in which 1,2,4-oxadiazole derivatives were utilized as the core active structure within numerous applications. Additionally, the preparation methods for substituted 1,2,4-oxadiazole derivatives are elaborated upon, and their potential value within agrochemistry is discussed.
含氮、氧的杂环已被纳入各种已批准的农药和农药候选物中。当代作物保护中持续存在的挑战在于不断寻求具有杀虫特性的新型含氮、氧杂环化合物。其中，1,2,4-恶二唑骨架是新农药发现和开发中研究最广泛的杂环之一。本综述重点阐述自2012年以来所采用的分子设计策略，并突出1,2,4-恶二唑衍生物的生物活性。在这个时间范围内，噻唑锌和氟苯恶二唑嗪已成为突出的例子，其中1,2,4-恶二唑衍生物在众多应用中被用作核心活性结构。此外，还阐述了取代1,2,4-恶二唑衍生物的制备方法，并讨论了它们在农业化学中的潜在价值。
