2-(4-芳基噻唑-2-基)-3-羟基丙烯腈类化合物的合成及其生物活性

为了寻找新的含2-噻唑基丙烯腈结构的先导化合物,利用2-(4-芳基噻唑-2-基)乙腈与酰氯在吡啶或氢化钠存在下反应,合成了9个2-(4-芳基噻唑-2-基)-3-羟基丙烯腈类化合物,其中8个为新化合物,利用1H NMR、MS和元素分析对其结构进行了表征。初步的生物活性测定结果表明,部分化合物在供试浓度下具有一定的杀虫、杀菌活性,其中化合物 5f 在100 mg/L下对棉花枯萎病菌Fusarium oxysporium的抑制率超过90%,化合物 5e 在250 mg/L下对蚕豆蚜Aphis fabae的致死率达95%。毒力测定结果表明, 5e 对蚕豆蚜的活性优于对照化合物2- -3-羟基-3- 丙烯腈( 6 )。

Synthesis and Biological Activity of 2-(4-Arylthiazol-2-yl)-3-hydroxyacrylonitrile

In order to find novel 2-(2-thiazolyl)acrylonitrile lead compounds,nine 2-(4-arylthiazol-2-yl)-3-hydroxyacrylonitriles were synthesized by reaction of 2-(4-aryllthiazol-2-yl)acetonitrile and acyl chloride in presence of pyridine or sodium hydride.Their structures were comfirmed by ¹H NMR,MS and elemental analysis.The preliminary bioassay indicated that some of the compounds have some insecticidal and fungicidal activity,especially the inhibition rate of compound 5f against Fusarium oxysporium was above 90% at 100 mg/L and the mortality rate of compound 5e against Aphis fabae was about 95% at 250 mg/L.The comparative determining on the toxicity of Aphis fabae indicated that the toxicity of compound 5e was better than compound 6 .