Design, Synthesis, and Antifungal Evaluation of 8-Hydroxyquinoline Metal Complexes against Phytopathogenic Fungi
作者:Xiao-Dan Yin、Kun-Yuan Ma、Yu-Ling Wang、Yu Sun、Xiao-Fei Shang、Zhong-Min Zhao、Ren-Xuan Wang、Yong-Jia Chen、Jia-Kai Zhu、Ying-Qian Liu
DOI:10.1021/acs.jafc.0c01322
日期:2020.10.7
production, food security, and human health globally, and novel antifungal agents with simple chemical scaffolds and high efficiency are needed. In this study, we designed and synthesized 38 8-hydroxyquinoline metal complexes and evaluated their antifungal activities. The results showed that most of the tested compounds possessed remarkable in vitro antifungal activity. Especially, compound 1e exhibited the
植物病原性真菌感染已成为全球农业生产,粮食安全和人类健康的主要威胁,因此需要具有简单化学支架和高效能的新型抗真菌剂。在这项研究中,我们设计和合成了38种8-羟基喹啉金属配合物,并评估了它们的抗真菌活性。结果表明,大多数测试化合物具有显着的体外抗真菌活性。特别是,化合物1E显示出所有的目标化合物中的最高抗真菌效力,用EC 50个的值0.0940,0.125,2.95和5.96微克/毫升,分别针对菌核病,灰霉病,禾谷镰刀菌以及Magnaporthe oryzae。初步的机理研究表明,化合物1e可能引起核盘菌的菌丝体异常,细胞膜通透性变化,细胞内含物泄漏以及抑制核盘菌形成和萌发。此外,化合物1e对核盘菌的体内抗真菌活性的结果表明1e具有比阳性对照嘧菌酯更高的疗效。因此,化合物1e有望成为开发新型抗真菌剂的新型主导结构。