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

摘要: 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50 mg/L时对淡色库蚊Culex pipiens pallens的致死率达到100％; C-3、C-6、C-15 在100 mg/L对稗草Echinochloa crusgalli Link、马唐Digitaria sanguinalis、苋菜Ambrosia tricolor Linn的白化度大于80％。

Abstract: 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%.