2-苄硫基烟酰胺类衍生物的合成及生物活性

Synthesis and Bioactivity of 2-Benzylsulfanyl Nicotinamide Derivatives

以2-苄硫基烟酸为原料,设计并合成了26个2-苄硫基烟酰胺类化合物,其化学结构经核磁共振氢谱和元素分析确证。初步的生物活性测定结果表明,该类化合物具有一定的杀虫及除草活性。其中C-9、C-10、C-11在50mg/L时对淡色库蚊Culex pipiens pallens的致死率达到100%;C-3、C-6、C-15在100mg/L对稗草Echinochloa crusgalliLink、马唐Digitaria sanguinalis、苋菜Ambrosia tricolorLinn的白化度大于80%。

In search for novel pesticides with high effects, high selectivity and low toxicity, 26 compounds belong to 2-benzylsulfanyl nicotinamide derivatives were designed and synthesized starting from 2-benzylsulfanyl nicotinic acid. Their chemical structures were confirmed by 1H NMR and elemental analysis. Preliminary bioassays showed that some compounds exhibited certain insecticidal and herbicidal activities. The mortality of Culex pipiens pallens from C-9, C-10 and C-11 at the concentration of 50 mg/L reached 100%. The albino rate of C-3, C-6, C-15 to Echinochloa crusgalli, Digitaria sanguinalis ,Ambrosia tricolor and Brassica alboglabra at the concentration of 100 mg/L was above 80%.