Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran 1417614411, Iran.
Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran 1417614411, Iran.
J Agric Food Chem. 2024 Jul 17;72(28):15427-15448. doi: 10.1021/acs.jafc.4c02187. Epub 2024 Jul 5.
With fungal diseases posing a major threat to agricultural production, the application of fungicides to control related diseases is often considered necessary to ensure the world's food supply. The search for new bioactive agents has long been a priority in crop protection due to the continuous development of resistance against currently used types of active compounds. Heterocyclic compounds are an inseparable part of the core structures of numerous lead compounds, these rings constitute pharmacophores of a significant number of fungicides developed over the past decade by agrochemists. Among heterocycles, nitrogen-based compounds play an essential role. To date, diazole (imidazole and pyrazole) and diazine (pyrimidine, pyridazine, and pyrazine) derivatives make up an important series of synthetic fungicides. In recent years, many reports have been published on the design, synthesis, and study of the fungicidal activity of these scaffolds, but there was a lack of a comprehensive classified review on nitrogen-containing scaffolds. Regarding this issue, here we have reviewed the published articles on the fungicidal activity of the diazole and diazine families. In current review, we have classified the molecules synthesized so far based on the size of the ring.
由于真菌病对农业生产构成重大威胁,因此为了确保世界粮食供应,常应用杀菌剂来控制相关疾病。由于目前使用的活性化合物的抗药性不断发展,因此寻找新的生物活性物质长期以来一直是作物保护的重点。杂环化合物是许多先导化合物核心结构中不可分割的一部分,这些环构成了过去十年间农用化学家开发的大量杀菌剂的药效团。在杂环化合物中,含氮化合物起着至关重要的作用。迄今为止,二唑(咪唑和吡唑)和二嗪(嘧啶、哒嗪和吡嗪)衍生物构成了重要的一系列合成杀菌剂。近年来,已经发表了许多关于这些支架的设计、合成和杀菌活性研究的报告,但缺乏对含氮支架的全面分类综述。针对这一问题,我们在这里回顾了关于二唑和二嗪家族杀菌活性的已发表文章。在当前的综述中,我们根据环的大小对迄今为止合成的分子进行了分类。