Zhou Yuanxiang, Gong Chenyu, Sun Zhiling, Zeng Wei, Meng Kaini, An Youshan, Hu Yuzhi, Xue Wei
National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
ACS Omega. 2024 Apr 5;9(15):17297-17306. doi: 10.1021/acsomega.3c10294. eCollection 2024 Apr 16.
In order to discover novel compounds with excellent agricultural activities, novel flavonol derivatives containing 1,3,4-thiadiazole were synthesized and evaluated for their antifungal activities. The bioassay results showed that some of the target compounds had good antifungal activities against , sp. and in vitro. It is worth noting that the half-effective concentration (EC) value of against was 2.4 μg/mL, which was obviously superior to that of azoxystrobin (21.7 μg/mL). The curative activity of at 200 μg/mL (79.9%) was better than that of azoxystrobin (59.1%), and its protective activity (90.9%) was better than that of azoxystrobin (83.9%). Morphological studies by using scanning electron microscopy and fluorescence microscopy revealed that could affect the normal growth of mycelium. In addition, the mechanism of action studies indicated that could affect the integrity of cell membranes by inducing the production of endogenous reactive oxygen species and the release of the malondialdehyde content, leading to membrane lipid peroxidation and the release of cell contents. The inhibitory activity of flavonol derivatives containing 1,3,4-thiadiazole on plant fungi is notable, offering significant potential for the development of new antifungal agents.
为了发现具有优异农业活性的新型化合物，合成了含1,3,4 - 噻二唑的新型黄酮醇衍生物，并对其抗真菌活性进行了评估。生物测定结果表明，部分目标化合物在体外对、、等菌株具有良好的抗真菌活性。值得注意的是，对的半数有效浓度（EC）值为2.4μg/mL，明显优于嘧菌酯（21.7μg/mL）。在200μg/mL时的治疗活性（79.9%）优于嘧菌酯（59.1%），其保护活性（90.9%）也优于嘧菌酯（83.9%）。通过扫描电子显微镜和荧光显微镜进行的形态学研究表明，能够影响的菌丝体正常生长。此外，作用机制研究表明，可通过诱导内源性活性氧的产生和丙二醛含量的释放来影响细胞膜的完整性，导致膜脂过氧化和细胞内容物的释放。含1,3,4 - 噻二唑的黄酮醇衍生物对植物真菌的抑制活性显著，为开发新型抗真菌剂提供了巨大潜力。
