3,4-二氯异噻唑-5-甲酰胺衍生物的合成及生物活性
Synthesis and biological activity of 3,4-dichloroisothiazole-5-carboxylic amides
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摘要: 异噻唑类杂环化合物具有广泛的生物活性。为了扩大先导结构的发现范围,以3,4-二氯异噻唑-5-甲酸为原料合成了10个未见文献报道的3,4-二氯异噻唑-5-甲酰胺衍生物;其结构经核磁共振氢谱、红外光谱和元素分析确证。初步生物测试结果表明,化合物Ⅲe对9种病原真菌表现出了广谱的抑菌活性,在50 μg/mL下其抑制率均超过50%;在100 μg/mL下,大部分化合物展现了较好的抗烟草花叶病毒(tobacco mosaic virus,TMV)或诱导烟草抗TMV活性,其中化合物Ⅲa和Ⅲi的诱导活性分别为41.88%和42.92%。Abstract: Isothiazole based heterocyclic compounds had various biological activities.In order to enlarge the library of novel elicitor lead with broad spectrum of highly systemic acquired resistance,a series of 3,4-dichloroisothiazole-5-carboxylic amides were synthesized by the reaction of carboxylic acid chlorination and condensation with 3,4-dichloroisothiazole-5-carboxylic acid as starting materials.All the ten novel compounds synthesized were confirmed by 1H NMR,IR and elemental analysis.Biological screening indicated that,compound Ⅲe presented broad-spectrum of fungicidal activity at 50 μg/mL against nine fungi with inhibition above 50%.Most compounds had good anti-tobacco mosaic virus(TMV) activity or systemic acquired resistance for tobacco against TMV at 100 μg/mL,among them,compound Ⅲa and Ⅲi exhibited 41.88% and 42.92% of good systemic acquired resistance for tobacco against TMV respectively.
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