CAJ | 학술논문

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~1H NMR、~(13)C 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.
이대추분정위원료,통과다보반응합성료일계렬3-(마람분기)-5-취대-1,2,4-이오서류화합물화3-(마람분기)-5-취대-4,5-이경-1,2,4-오이서류화합물,병용~1H NMR、~(13)C NMR화MS진행료결구학증.저사화합물대측시적부분혁란씨양성균,여금황색포도구균、내갑양서림금황색포도구균、표피포도구균、분장구균현시출일정적항균활성,단여오서완동류상시약물리내서알상비,항균활성유명현하강.저일결과표명대우화합물적항균활성,1,2,4-오이서잡배불여오서완동결구유효.
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,~(13)C NMR and HRMS.These compounds showed certain antibacterial activities against a panel of tested Gram-positive bacteria,including Staphylococcus aureus,methicillin-resistant Staphylococus aureus,Staphylococcus epidermis,Enterococcus faecalis and Escherichia coil.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.