Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing 210095, China.
Molecules. 2022 Oct 14;27(20):6904. doi: 10.3390/molecules27206904.
Coumarin compounds have a variety of biological activities such as anti-tumor, anti-coagulation, anti-HIV, anti-fungal, and insecticidal. Amide and sulfonamide compounds have been used as fungicides for half a century, and dozens of varieties have been developed so far. This study focused on the introduction of carboxamide and sulfonamide moieties in a coumarin core to discover novel derivatives. Based on this strategy, we synthesized two series of novel carboxamide and sulfonamide substituted coumarin derivatives, and their fungicidal activity was also investigated. Some designed compounds possessed potential activities against six phytopathogenic fungi in the primary assays, highlighted by compound . Compound exhibited stronger fungicidal activity against (EC = 20.52 µg/mL) and will be the lead structure for further study.
香豆素类化合物具有多种生物活性，如抗肿瘤、抗凝血、抗 HIV、抗真菌和杀虫。酰胺和磺酰胺类化合物作为杀菌剂已经使用了半个世纪，目前已经开发出几十种。本研究集中在香豆素核心中引入羧酰胺和磺酰胺基团，以发现新型衍生物。基于这一策略，我们合成了两类新型的羧酰胺和磺酰胺取代香豆素衍生物，并对其杀菌活性进行了研究。一些设计的化合物在初步试验中对六种植物病原菌具有潜在的活性，其中化合物 表现出更强的杀菌活性，对 （EC=20.52μg/mL）的抑制活性最强，将成为进一步研究的先导结构。
