3--氟4-(2-芳基噻-唑4-基)苯基唑烷酮类化合物的合成及抗菌活性

Synthesis and antibacterial activities of 3-fluoro-4-(2-arylthiazol-4-yl)phenyl oxazolidinone derivatives

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-fluoro-4-（2-arylthiazol-4-yl） phenyl oxazolidinone deriva- tives and primarily evaluate their in vitro antibacterial activities. Methods A new synthetic route was used to synthesize the title compounds starting from 2-chloromethyloxirane and 3-fluorophenyl isocyanate and their in vitro antibacterial activities were examined using Mueller-Hinton broth dilution method. Results and Conclusion Fourteen new compounds are prepared and their structures are confirmed by ^1H-NMR and MS. Ten of them show antibacterial activities. Compounds IXc and Xc display promising activities and are worth further study.