Yin Xiao-Dan, Sun Yu, Lawoe Raymond Kobla, Yang Guan-Zhou, Liu Ying-Qian, Shang Xiao-Fei, Liu Hua, Yang Yu-Dong, Zhu Jia-Kai, Huang Xiao-Ling
School of Pharmacy, Lanzhou University Lanzhou 730000 People's Republic of China
Lanzhou Institute of Husbandry and Pharmaceutical Sciences, Chinese Academy of Agricultural Sciences 335 Jiangouyan Lanzhou 730050 P. R. China.
RSC Adv. 2019 Sep 24;9(52):30087-30099. doi: 10.1039/c9ra05712a. eCollection 2019 Sep 23.
Phytopathogenic fungi have become a serious threat to the quality of agricultural products, food security and human health globally, necessitating the need to discover new antifungal agents with chemical scaffolds and high efficiency. A series of 8-hydroxyquinoline derivatives were designed and synthesized, and their antifungal activity was evaluated against five phytopathogenic fungi. assays revealed that most of the tested compounds remarkably impacted the five target fungi and their inhibitory activities were better than that of the positive control azoxystrobin. Compound 2, in particular, exhibited the highest potency among all the tested compounds, with an EC of 0.0021, 0.0016, 0.0124, 0.0059 and 0.0120 mM respectively against , , , and , followed by compound 5c. The morphological observations of optical microscopy and scanning electron microscopy revealed that compounds 2 and 5c caused mycelial abnormalities of . Futhermore, the results of antifungal activity of compounds 2 and 5c against showed that 5c possessed stronger protective and curative activity than that of 2, and the curative effects of 5c at 40 and 80 μg mL (84.18% and 95.44%) were better than those of azoxystrobin (77.32% and 83.59%). Therefore, compounds 2 and 5c are expected to be novel lead structures for the development of new fungicides.
植物病原真菌已成为全球农产品质量、粮食安全和人类健康的严重威胁，因此需要发现具有新型化学结构骨架和高效性的新型抗真菌剂。设计并合成了一系列8-羟基喹啉衍生物，并对其针对五种植物病原真菌的抗真菌活性进行了评估。试验表明，大多数测试化合物对五种目标真菌有显著影响，其抑制活性优于阳性对照嘧菌酯。特别是化合物2在所有测试化合物中表现出最高的活性，对番茄灰霉病菌、瓜果腐霉菌、辣椒疫霉菌、小麦赤霉病菌和玉米大斑病菌的EC50分别为0.0021、0.0016、0.0124、0.0059和0.0120 mM，其次是化合物5c。光学显微镜和扫描电子显微镜的形态学观察表明，化合物2和5c导致番茄灰霉病菌的菌丝体异常。此外，化合物2和5c对番茄灰霉病菌的抗真菌活性结果表明，5c具有比2更强的保护和治疗活性，5c在40和80 μg/mL时的治疗效果（84.18%和95.44%）优于嘧菌酯（77.32%和83.59%）。因此，化合物2和5c有望成为开发新型杀菌剂的新型先导结构。
