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为了发现更多抑菌活性优于抗菌药物盐酸氯康唑的化合物,在盐酸氯康唑的结构基础上,设计、合成了其类似物,并进行了抑菌活性测定。以芝麻酚为原料,经过酰化、1,2,4-三氮唑基团的引入以及醚化3步反应,合成了19个新型氯康唑类似物4a~4s。所有目标化合物的结构均经过~1H NMR、~(13)C NMR和ESI-MS等确认。采用抑制菌丝生长速率法测定了目标化合物对水稻稻瘟病菌、番茄早疫病菌、马铃薯干腐病菌、玉米弯孢病菌、烟草赤星病菌、小麦赤霉病菌和棉花枯萎病菌7种植物源病原真菌的抑制活性,并进一步测定了部分化合物的EC_(50)值。结果显示,在50μg/m L时,大多数目标化合物对供试菌株表现出不同程度的抑制作用。其中,化合物4d和4m对番茄早疫病菌的EC_(50)值分别为6.28和4.61μg/m L,4m对烟草赤星病菌的EC_(50)值3.58μg/m L,与对照药剂腈菌唑(对番茄早疫病菌和烟草赤星病菌的EC_(50)值分别为1.63和1.05μg/m L)在同一数量级,具有开发为新型抗菌药物的潜能。
In order to find out more antibacterial activity than the antibacterial drug cloconazole hydrochloride compound, based on the structure of cloconazole hydrochloride, the design and synthesis of its analogues, and the determination of antibacterial activity. Nineteen novel cloconazole analogues 4a ~ 4s were synthesized from sesamol by acylation, 1,2,4-triazole group introduction and etherification three-step reaction. The structure of all the target compounds were confirmed by ~ 1H NMR, ~ (13) C NMR and ESI-MS. The inhibitory rates of mycelium growth on the seven pathogenic fungi of Magnaporthe grisea, Alternaria solani, Alternaria solani, Curvularia lunata, Fusarium oxysporum, Fusarium graminearum and Fusarium oxysporum were determined. The inhibitory activity of some compounds was also determined. The results showed that at 50μg / mL, most of the target compounds showed different degrees of inhibition on the tested strains. Among them, the EC50 values of compound 4d and 4m against Alternaria solani were 6.28 and 4.61μg / m L, respectively, and the EC50 value of 4m against Alternaria solani was 3.58μg / m L, (EC 50 values of 1.63 and 1.05 μg / mL for Alternaria solani and Alternaria solani) were of the same order of magnitude and had the potential to develop as novel antibacterial agents.