2-酰氨基苯并噻唑-7-甲酸甲酯类化合物的合成及其抗病诱导活性

Synthesis and Induced Resistance Activities of Methyl 2-amidobenzothiazole-7-carboxylates

摘要: 以3-氨基苯甲酸为原料,经酯化、关环、酰基化等反应合成了22个未见文献报道的2-酰氨基苯并噻唑-7-甲酸甲酯类化合物,其结构经过IR、1H NMR和元素分析确认。初步的生物活性测定结果表明:在1 000mg/L浓度下,部分化合物对黄瓜灰霉病菌Botrytis cinerea具有一定的离体抑制活性,抑制率为60%~73%;化合物Ⅲ-4、Ⅲ-13、Ⅲ-19、Ⅲ-20的活体抑菌活性(抑制率)分别为83.0%、65.0%、88.9%和74.8%,均高于相应的离体活性,表现出一定的抗病诱导活性。

Abstract: Twenty two novel methyl 2-amidobenzothiazole-7-carboxylates were prepared.The structures were confirmed by elemental analysis,1H NMR and IR.The preliminary bioassay showed that some of them had good fungicidal activities against Botrytis cinerea in vitro at the concentration of 1 000 mg/L,and the inhibition rate were between 60%~73%.The inhibition rate of compounds Ⅲ-4,Ⅲ-13,Ⅲ-19 and Ⅲ-20 were 83.0%,65.0%,88.9% and 74.8% in vivo,respectively.It was higher than that of in vitro.The results showed that some of the compounds have induced resistance activities.