Abstract：
24 chalcone derivatives containing 1,3,4-thiadiazole were synthesized. The results of bioactivity tests indicated that some of the target compounds exhibited superior antifungal activities in vitro. Notably, the EC50 value of D4 was 14.4 μg/mL against Phomopsis sp, which was significantly better than that of azoxystrobin (32.2 μg/mL) and fluopyram (54.2 μg/mL). The in vivo protective activity of D4 against Phomopsis sp on kiwifruit (71.2 %) was significantly superior to azoxystrobin (62.8 %) at 200 μg/mL. The in vivo protective activities of D4 were 74.4 and 57.6 % against Rhizoctonia solani on rice leaf sheaths and rice leaves, respectively, which were slightly better than those of azoxystrobin (72.1 and 49.2 %) at 200 μg/mL. Scanning electron microscopy (SEM) results showed that the mycelial surface collapsed, contracted and grew abnormally after D4 treatment. Finally, the results were further verified by in vivo antifungal assay, fluorescence microscopy (FM) observation, determination of relative conductivity, membrane lipid peroxidation degree assay, and determination of cytoplasmic content leakage. Molecular docking results suggested that D4 could be a potential SDHI.
摘要：
合成了24个含1,3,4-噻二唑的查耳酮衍生物。生物活性测试结果表明，一些目标化合物在体外表现出优异的抗真菌活性。值得注意的是,D4的EC50值为14.4µg/mL，其显着优于氮菌酯（32.2µg/mL）和氟吡仑（54.2µg/mL）。在200µg/mL时，D4对猕猴桃的体内保护活性（71.2％）明显优于唑酯酯（62.8％）。D4对水稻叶鞘和水稻叶片的体内保护活性分别为74.4和57.6％，分别,在200µg/mL时，略好于唑菌酯（72.1％和49.2％）。扫描电镜(SEM)结果表明菌丝表面塌陷,D4治疗后异常收缩和生长。最后,结果通过体内抗真菌试验进一步验证，荧光显微镜（FM）观察，相对电导率的测定，膜脂过氧化程度测定，并测定细胞质内容物渗漏。分子对接结果表明D4可能是潜在的SDHI。
