新3,5-二取代噁唑烷酮抗菌剂的合成及其体外抑菌活性

Synthesis and in vitro antibacterial activities of new 3,5-disubstituted oxazolidinone compounds

目的 设计、合成唑烷酮新化合物并测定其体外抑菌活性。方法 对文献方法进行了改进 ,在文献报道的构效关系基础上 ,设计、合成唑烷酮新化合物并测定体外抑菌活性。结果 合成了 39个新化合物 ,其中目标物 1 8个 ,其结构经IR ,1 HNMR ,MS等方法确证。 1 6个化合物显示出较好的抑菌活性 ,其中化合物 9,1 0 ,1 0b对 4种试验菌的MIC50 和MIC90 值小于或接近 4种对照药 ,化合物 9a和 1 1c没有抑菌活性。结论 化合物 9,1 0和 1 0b值得进一步研究。

Aim To design and synthesize new oxazolidinone antibacterial agents. Methods The synthetic method reported in literature has been modified and new 3,5 disubstituted oxazolidinone compounds were synthesized on the basis of SAR reported in the literature and their antibacterial activities in vitro were determined. Results Eighteen new objective compounds were synthesized, and their structures were determined by IR, 1HNMR and FAB MS. Within the eighteen new objective compounds, sixteen compo...