新型3,5-二取代恶唑烷酮类化合物的合成及其体外抗菌活性
[Synthesis and in vitro antibacterial activities of new 3,5-disubstituted oxazolidinone compounds].
作者信息
Meng Qing-guo, Wang Qi, Liu Jun
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
出版信息
Yao Xue Xue Bao. 2003 Oct;38(10):754-9.
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 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.
CONCLUSION
Compounds 9, 10 and 10b are worthy to be intensively studied.
目的
设计并合成新型恶唑烷酮类抗菌剂。
方法
对文献报道的合成方法进行改进，依据文献报道的构效关系合成新型3,5-二取代恶唑烷酮化合物，并测定其体外抗菌活性。
结果
合成了18个目标化合物，通过红外光谱、核磁共振氢谱和快原子轰击质谱确定了它们的结构。在这18个目标化合物中，16个化合物具有体外抗菌活性，化合物9、10和10b的体外抗菌活性优于环丙沙星（CIP）、舒他西林（Sul）和万古霉素（VCO）。化合物9a和11c在体外完全没有抗菌活性。
结论
化合物9、10和10b值得深入研究。
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