1，2，4-噁二唑类化合物的合成及抗菌活性研究  

Synthesis and antibacterial activity of 1,2,4-oxadiazole derivatives

作　　者：陈东亮[1] 初文毅[1] 鄢明[1] 

机构地区：[1]中山大学药学院,中山大学精细化工与合成药物工业研究院,广东广州510006

出　　处：《化学研究与应用》2010年第2期176-181,共6页Chemical Research and Application

基　　金：国家自然科学基金资助项目(20772160);珠海市科技计划资助项目

摘　　要：以对溴苯腈为原料,通过多步反应合成了一系列3-(吗啉苯基)-5-取代-1,2,4-异噁唑类化合物和3-(吗啉苯基)-5-取代-4,5-二氢-1,2,4-噁二唑类化合物,并用1HNMR、13C NMR和MS进行了结构确证。这些化合物对测试的部分革兰氏阳性菌,如金黄色葡萄球菌、耐甲氧西林金黄色葡萄球菌、表皮葡萄球菌、粪肠球菌显示出一定的抗菌活性,但与噁唑烷酮类上市药物利奈唑胺相比,抗菌活性有明显下降。这一结果表明对于化合物的抗菌活性,1,2,4-噁二唑杂环不如噁唑烷酮结构有效。A series of 3-morpholinophenyl-5-substituted-1,2,4-oxadiazole and 3-morpholinophenyl-5-substituted-4,5-dihydro-1, 2, 4-oxadiazole derivatives were prepared. Their structures were confirmed by 1H NMR,13C NMR and HRMS. These compounds showed certain antibacterial activities against a panel of tested Gram-positive bacteria,including Staphylococcus aureus, methieillinresistant Staphylococcus aureus, Staphylococcus epidermis, Enteroeoecus faecalis and Escherichia coll. However the antibacterial activities were significantly lower than that of linezolid which was the first oxazolidinone antibacterial into the market. The results implied that the 1,2,4-oxadiazole motif was inferior to the oxazolidinone motif for the antibacterial activity.

关 键 词：1 2 4-噁二唑 合成 抗菌活性 

分 类 号：O629.9[理学—有机化学]