Synthesis and evaluation of imidazo[1,2-a]quinoxaline derivatives as potential antifungal agents against phytopathogenic fungi
作者:Taigui Ma、Xu Zhong、Ya Yang、Wenjing Liu、Bing Guo、Judi Fan、Lei Tang、Lingling Fan、Yong Li
DOI:10.1007/s11030-023-10739-y
日期:——
potential agricultural antifungal agents, various kinds of imidazo[1,2-a]quinoxaline derivatives were designed, and synthesized from available and inexpensive reagents. Their antifungal activities were first evaluated against ten typical phytopathogenic fungi. The in vitro antifungal activity showed that some compounds exhibited more obvious broad-spectrum fungicidal activity than the two commercially-available
为了发现新颖有效的潜在农业抗真菌剂,设计了各种咪唑[1,2-a]喹喔啉衍生物,并用现有和廉价的试剂合成。首先针对 10 种典型的植物病原真菌评估了它们的抗真菌活性。体外抗真菌活性表明,一些化合物比两种市售杀菌剂百菌清和噻沙唑表现出更明显的广谱杀菌活性。Mali 和 Botrytis cinerea 菌株对 10 多种化合物的 EC50 值为 1.4-27.0 μg/mL,表现出最高的敏感性。化合物 5c 和 5f 分别对苹果笙草 (EC50 = 5.6 μg/mL) 和茄子镰刀菌 (EC50 = 5.1 μg/mL) 显示出最有希望的抑制作用。关于作用机制的初步研究表明,咪唑[1,2-a]喹喔啉骨架可能通过破坏菌丝分化、孢子萌发和胚芽管生长来发挥其抗真菌作用。此外,细胞实验结果表明,这些靶标化合物对 BV2 细胞具有良好的安全性。总体而言,化合物 5c 和 5f 可以被认为是针对特定真菌的