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为了寻求和开发新的基于天然产物的杀螨剂,在明确姜黄素具有杀螨活性,且其结构中的双羰基并非杀螨活性关键基团的基础上,设计并合成了15个姜黄素异噁唑和吡唑衍生物,其结构均经红外光谱、核磁共振氢谱和质谱分析确认。生物活性测定结果表明:几乎所有的目标化合物对朱砂叶螨Tetranychus cinnabarinus和柑橘全爪螨Panonychus citri均表现出了比先导化合物姜黄素更优异的触杀活性,其中化合物4和11的活性最为突出。处理48 h后,化合物4对朱砂叶螨和柑橘全爪螨的LC50值分别为333.0和156.0 mg/L,其毒力是姜黄素的6.35和4.56倍,11的LC50值分别为478.4和144.7 mg/L,毒力是姜黄素的4.42和4.92倍;相应地处理72 h后,4的LC50值分别为115.0和84.9 mg/L,其毒力是姜黄素的5.02和1.43倍,11的LC50值分别为91.0和68.7 mg/L,毒力是姜黄素的6.35和1.77倍。化合物4和11可作为进一步开发研究的具有杀螨活性的候选化合物。
In order to find out and develop new acaricides based on natural products, 15 curcumin derivatives were designed and synthesized on the basis of specifying the acaricidal activity of curcumin and the double carbonyl group in its structure as the key group of acaricidal activity. Oxazole and pyrazole derivatives, the structure of which are confirmed by IR, 1H NMR and MS. The results of bioassay showed that almost all of the target compounds showed more excellent activity than the lead compounds curcumin Tetranychus cinnabarinus and Panonychus citri, of which compounds 4 and 11 were the most prominent. After 48 h of treatment, the LC50 values of compound 4 against Tetranychus cinnabarinus and Citrus red mite were 333.0 and 156.0 mg / L, respectively. The virulence of compound 4 was 6.35 and 4.56 times higher than that of curcumin, and the LC50 values of 11 were 478.4 and 144.7 mg, respectively / L and 4.42 and 4.92 folds of curcumin respectively. LC50 values of 4 at 115 h and 84.9 mg / L, respectively, after treatment for 72 h were 5.02 and 1.43 times higher than those of curcumin and LC50 values of 11 91.0 and 68.7 mg / L, respectively. The virulence was 6.35 and 1.77 folds of curcumin. Compounds 4 and 11 can be used as candidate compounds for acaricidal activity for further development.