井冈羟胺A酯类衍生物的酶法合成及其生物活性

Enzymatic synthesis and biological activities of validoxylamine A ester derivatives

井冈羟胺A(validoxylamine A)作为重要的生物农药中间体具有抑菌和杀虫活性。为开发新型绿色农药,以井冈羟胺A作为先导化合物,通过脂肪酶催化酯化反应,合成了9个未见文献报道的井冈羟胺A酯类衍生物,通过核磁共振氢谱、碳谱以及高分辨质谱对其结构进行了表征。生物活性测定结果表明:大部分目标化合物对立枯丝核菌Rhizoctonia solani具有抑制活性,其中化合物Ⅰ的抑制效果最好,EC_(50)值为13.03μmol/L;化合物Ⅶ在500 mg/L下对豆蚜Aphis craccivora的致死率为64.60%。该类衍生物具有一定的抑菌、杀虫活性,有进一步研究的价值。

Validoxylamine A is an important biopesticide intermediate with bacteriostatic and insecticidal activities.To discover new green pesticides,9 novel compounds were synthesized by lipase esterification reaction using validoxylamine A as the lead compound.Their structures were characterized byⅠH NMR,^(13)C NMR and HRMS.The biological activities results showed that most of those compounds retained their inhibitory activity against Rhizoctonia solani.CompoundⅠhad the best inhibitory effect,with the EC_(50) value of 13.03μmol/L.CompoundⅦhad a lethality of 64.60%to Aphis craccivora at 500 mg/L.This class of derivatives has fungicidal and insecticidal activities and is worthy of further study.