2-(3,4,5-三苄氧基苯基)-5-取代硫醚-1,3,4-噁二唑类化合物的合成及生物活性研究

Synthesis and Biological Activities of 2-(3,4,5-Tribenzyloxyphenyl)-5-alkylthio-1,3,4-oxadiazole Derivatives

以没食子酸为起始原料,经酯化、醚化、酰肼化、关环和硫醚化五步反应合成了9个新型的2-(3,4,5-三苄氧基苯基)-5-取代硫醚-1,3,4-噁二唑类化合物6a^6i,其结构经元素分析I、R1、H NMR和MS表征.初步的生物活性测试结果表明,所合成的化合物均表现出不同程度的抑菌活性,其中,6h的活性最好,在50 mg/L浓度下对棉花枯萎病菌和黄瓜灰霉病菌的抑制率达90%以上.

Nine novel 2-（3,4,5-tribenzyloxyphenyl）-5-alkylthio-1,3,4-oxadiazole derivatives （6a - 6i） were synthesized based on the starting material gallic acid by five steps： esterification, etherification, hydrazidation, cyelization, and thioetherification. All compounds synthesized are confirmed by elemental analysis, IR, ^1H NMR and MS spectra Preliminary bioassay indicates that some compounds display excellent fungicidal activity to some extent, among them the compound 6 h exhibited higher than 90 % inhibition effect against Fusarium oxysporum and Botrytis cinereapers in dosage of 50 mg/L.