Synthesis and Antibacterial Activity of (S)-5-(Heterocycle Methylene) -3-(3-Fluoro-4-morpholin-4-yl-phenyl)-Oxazolidin-2-one Derivatives

(S)-5-(氮杂环亚甲基)-3-(3-氟-4-吗啉-4-基-苯基)噁唑烷-2-酮衍生物的合成及抗菌活性(英文)

Aim To study the structure-activity relationship of antibacterial oxazolidinone derivatives. Methods Seven （S） -5- （ heterocycle methylene） -3- （3-fluoro-4-morpholin-4-yl-phenyl） -oxazoli- din-2-ones were synthesized by the substitution of （S）-[ 3-（3-fluoro-4-morpholin-4-yl-phenyl）-oxazohdin-2-one-5-yl]-methanol mesylate with some secondary amines and the structures of the product were confirmed by ^1H NMR and elemental analyses or MS. Results None of the seven compounds showed potent activity against the tested 20 strains of bacteria in vitro. Conclusion The replacement of 5- acetylaminometyl of Linezolid by 5-（heterocycle methylene） lost the antibacterial activity.

目的研究具有抗菌作用的噁唑烷酮衍生物的构效关系。方法由(S)-[3-(3-氟-4-吗啉-4-基-苯基)噁唑烷-2-酮-5-基]-甲醇甲磺酸酯和仲胺的取代反应合成了7个(S)-5-氮杂环亚甲基-3-(3-氟-4-吗啉-4-基-苯基)噁唑烷-2-酮衍生物,其结构通过1HNMR和元素分析或质谱确证。结果所合成的7个化合物对所测的20株细菌均没有明显的体外抗菌活性。结论用氮杂环亚甲基取代吗啉噁酮的5位乙酰胺甲基降低化合物的抗菌活性。