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目的设计合成具有手性吡咯烷侧环的唑烷酮类化合物,并考察其体外抗菌活性。方法以手性脯氨酸和34,-二氟硝基苯为原料,通过多步反应合成目标化合物;采用微量液体稀释法检测目标化合物的抗菌活性。结果与结论合成了8个新化合物,其结构经1H-NMR、MS谱确证。体外活性试验表明:由(R)-脯氨酸衍生的化合物7b对革兰阳性菌[金黄色葡萄球菌、表皮葡萄球菌以及耐甲氧西林金黄色葡萄球菌(MRSA)]具有良好的抑制活性,对革兰阴性菌具有较弱的抑制活性。由(S)-脯氨酸衍生的化合物7a的抗菌活性明显低于7b。研究结果表明,吡咯烷侧环的手性因素对抗菌活性具有显著影响。
OBJECTIVE To design and synthesize the oxazolidinones with chiral pyrrolidine side rings and investigate their in vitro antibacterial activity. Methods The chiral proline and 34, - difluoronitrobenzene as raw materials, the synthesis of the target compound by multi-step reaction; the use of trace liquid dilution method to detect the antibacterial activity of the target compound. Results and Conclusion Eight novel compounds were synthesized and their structures were confirmed by 1H-NMR and MS spectra. In vitro activity tests showed that compound 7b derived from (R) - proline had good inhibitory activity against Gram - positive bacteria [Staphylococcus aureus, Staphylococcus epidermidis and MRSA] Gram-negative bacteria have weaker inhibitory activity. The antibacterial activity of compound 7a derived from (S) -proline was significantly lower than that of 7b. The results show that the chirality of the pyrrolidine ring has a significant effect on the antibacterial activity.