【摘要】 为了发现具有良好生物活性的新型先导化合物,通过活性亚结构拼接方法,在保留噻唑菌胺、甲噻灵和噻氟菌胺等中的1,3-噻唑-5-羰基活性部分,将具有良好生物多样性的苯氧乙酸酯基团引入,设计合成了一系列含苯氧乙酸酯基团结构的1,3-噻唑类化合物.以β-酮酸酯和对羟基硫代苯甲酰胺为原料,经6步反应制得目标物,其结构经1H NMR,IR及高分辨质谱确证,并对该类化合物合成方法进行了探讨.初步生测结果表明,部分化合物对小麦赤霉表现出明显的抑制活性,在50μg/mL浓度下对小麦赤霉的抑制率达到52%.更多还原

【Abstract】 To find new lead compounds with muti-bioactivities,a series of novel 1,3-thiazole-5-carboxylic acid derivatives containing aryloxyacetate were designed via the method of linking active sub-structures,in which the aryloxyacetate with multi-bioactivity was combined to the 1,3-thiazole moiety of ethaboxam,metsulfovax and thifluzamide.The target compounds were synthesized from β-keto acid ester and 4-hydroxybenzothioamide in 6 steps.Their structures were confirmed by 1H NMR,IR and HRMS techniques.The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Fusarium graminearum,and the fungicidal activity of 1j is 52% at 50 μg/mL.更多还原