新3,5-二取代唑烷酮抗菌剂的合成及其体外抑菌活性新3,5-二取代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

摘要: 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18个，其结构经IR,¹HNMR,MS等方法确证。16个化合物显示出较好的抑菌活性，其中化合物9，10，10b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11c没有抑菌活性。结论化合物9，10和10b值得进一步研究。

Abstract: AimTo design and synthesize new oxazolidinone antibacterial agents.MethodsThe 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.ResultsEighteen new objective compounds were synthesized, and their structures were determined by IR, ¹HNMR and FAB-MS.Within the eighteen new objective compounds, sixteen compounds showed antibacterial activity in vitro and compound 9, 10 and 10b showed better antibacterial activities in vitro than ciprofloxacin (CIP), sultamicillin (Sul) and vancomycin (VCO). Compounds 9a and 11c have no antibacterial activity in vitro at all.ConclusionCompounds 9, 10 and 10b are worthy to be intensively studied.