2-(N-苯磺酰基吲哚-3-基)-3-N-酰基-5-苯基-1,3,4-噁唑啉类化合物抑菌活性研究

Antifungal Activities of 2-(N-Arylsulfonylindol-3-yl)-3-N-acyl-5-phenyl-1,3,4-oxadiazolines

为了研究2-(N-苯磺酰基吲哚-3-基)-3-N-酰基-5-苯基-1,3,4-噁唑啉类化合物中具有潜在应用价值的抑菌先导化合物。在0.1 g/L质量浓度下,采用菌丝生长速率法测定了14种2-(N-苯磺酰基吲哚-3-基)-3-N-酰基-5-苯基-1,3,4-唑啉类化合物对小麦赤霉病菌、白菜黑斑病菌、棉花枯萎病菌、水稻稻瘟病菌和烟草赤星病菌的室内抑菌活性。结果表明,化合物1~化合物14对所测5种植物病原菌均表现出不同程度的抑菌活性,其中化合物9和化合物14对小麦赤霉病菌、白菜黑斑病菌、棉花枯萎病菌、水稻稻瘟病菌和烟草赤星病菌5种植物病原菌活性较好,其抑制率分别为15.69%~31.08%和16.28%~29.41%,表现出一定的广谱抑菌活性。初步拟定将这2个化合物作为进一步衍生修饰的先导化合物。

In order to discover applicable lead compounds with antifungal activities from 2-（N-arylsulfonylindol-3-yl）- 3-N-acyl-5-phenyl-1,3,4-oxadiazolines. Fourteen 2-（N-arylsulfonylindol-3-yl）-3-N-acyl-5-phenyl-1,3,4-oxadiazolines were prepared, and their antifungal activities were evaluated against Fusarium 9raminearum, Alternaria brassieae, Fusarium oxysporium f. sp. Vasinfeetum synder et, Pyrieularia oryzae and Altemaria alternate by mycelium growth rate method in vitro at the concentration of 0.1 g/L, respectively. A preliminary structure-activity relationship was studied, compound 1- compound 14 showed different degrees of antifungal activities on five kinds of plant pathogenic fungi. Among all derivatives, compound 9 and compound 14 exhibited broad-spectrum antifungal activities against five kinds of plant pathogenic fungi, with the final inhibitory rates of 15.69%-31.08% and 16.28%-29.41%, respectively. Compound 9 and compound 14 could be considered as the lead compounds.