新型噁唑烷酮类化合物5-位侧链的结构改造及抗菌活性

Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activities

摘要: 目的对噁唑烷酮类化合物5-位侧链进行结构修饰与改造，并初步评价其体外抗菌活性。方法以间氟苯胺为原料，经9～12步反应合成目标化合物；采用二倍稀释法，测定目标化合物的体外抗菌活性。结果设计、合成了30个新化合物，其中目标化合物18个，其结构经^{1^{H NMR及MS等方法确证，11个化合物显示出不同程度的抗菌活性，化合物7a，9a和11a的活性较好。结论化合物7a，9a和11a值得进一步研究。}}

Abstract: AimTo modify the C-5 side chains of the oxazolidinone derivatives and evaluate their in vitro antibacterial activities preliminarily. MethodsThe title compounds were synthesized in 9-12 steps with the starting material 3-fluoroaniline and their in vitro antibacterial activities were examined by using Mueller-Hinton broth dilution method. ResultsThirty new compounds were designed and synthesized, in which eighteen novel title compounds were prepared and their structures were confirmed by ^{1^{H NMR and ESI-MS. Eleven compounds showed antibacterial activities to a certain extent, among them compounds 7a, 9a and 11a displayed promising activity. ConclusionCompounds 7a, 9a and 11a were worth further studying.}}