论文部分内容阅读
合成了一系列13个吡啶查尔酮衍生物,目标化合物的结构通过~1H NMR、~(13)C NMR和HRMS进行了确证.体外抗菌活性评价结果显示,其中的五个化合物对于革兰氏阳性金黄色葡萄球菌(ATCC 29213)表现出良好的抑制活性.为进一步评估活性,选取11株无重复的耐甲氧西林金黄色葡萄球菌(MRSA)临床株对上述5个化合物进行进一步的药效测评.数据显示,其中四个化合物对于MRSA表现出较好的抑菌活性,其中(E)-2-溴-N-{4-[3-(2-吡啶基)丙烯酰基]苯基}乙酰胺(5k)对MRSA的抑菌效力最为明显,其最小抑菌浓度(MIC)为4μg/m L.在安全性评价方面,对化合物5k进行红细胞毒性评价,结果显示化合物5k即使在1000μg/m L的浓度下对于红细胞也几乎不存在毒性.综合上述数据分析,吡啶查尔酮5k作为新型抗MRSA药物具有进一步研究的价值.
A series of 13 pyrazolone derivatives were synthesized and their structures were confirmed by ~ 1H NMR, ~ (13) C NMR and HRMS. The results of in vitro antibacterial activity evaluation showed that five of the compounds were effective against Gram Positive Staphylococcus aureus (ATCC 29213) showed good inhibitory activity.In order to further evaluate the activity of eleven non-repeated clinical strains of methicillin-resistant Staphylococcus aureus (MRSA) for the above five compounds for further efficacy The data showed that four of the compounds showed good antibacterial activity against MRSA. Among them, (E) -2-bromo-N- {4- [3- (2-pyridyl) acryloyl] phenyl} The inhibitory effect of amide (5k) on MRSA was the most obvious, with the MIC of 4μg / m L. The evaluation of erythrocytes on compound 5k in safety evaluation showed that even at 5μg / L concentration of erythrocytes is almost non-toxic.According to the above data analysis, pyridine chalcone 5k as a new anti-MRSA drug with further research value.