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目的设计并合成3--氟4-(2-芳基噻-唑4-基)苯基唑烷酮类化合物,初步评价其体外抗菌活性。方法以(R)-环氧氯丙烷和间氟苯基异氰酸酯为起始原料,通过新的合成路线制备了目标化合物;采用微量液体稀释法,测定目标化合物的体外抗菌活性。结果与结论合成了14个新化合物,其结构经1H-NMR、MS确认,10个化合物显示出不同程度的抗菌活性,化合物IXc和Xc的活性较好,有进一步研究的价值。
OBJECTIVE To design and synthesize 3-fluor 4- (2-arylthiazole-4-yl) phenyl oxazolidinones for preliminary evaluation of their antibacterial activity in vitro. Methods (R) - epichlorohydrin and m - fluorophenyl isocyanate as starting materials, the new synthetic route prepared by the target compound; trace liquid dilution method was used to determine the target compound in vitro antibacterial activity. RESULTS AND CONCLUSIONS A total of 14 new compounds were synthesized and their structures were confirmed by 1H-NMR and MS. The ten compounds showed different degrees of antibacterial activity, and the compounds IXc and Xc showed good activity and were further studied.