摘要
致力于开发头孢哌酮衍生物以应对细菌耐药性问题。通过系统化的合成路径研究,探讨了不同反应条件下头孢哌酮衍生物的合成收率和产物质量,包括反应温度、时间和物质添加量。优化条件为7-ACA添加量0.15 mol、反应温度25℃、反应时间2 h。优化条件下合成的头孢哌酮衍生物对金黄色葡萄球菌和大肠杆菌有显著的抗菌活性。同时通过抑菌圈直径测试和最小抑菌浓度(MIC)实验评估了合成化合物的抗菌效力。尽管与现有抗生素相比,抗菌效力有待提高,但在扩展抗菌谱和克服细菌耐药性方面具有较大潜力。对该化合物进行了表征及分析,并初步推测其分子式为C_(17)H_(19)N_(5)O_(5)S。
The study is dedicated to develop cephalosporin derivatives to overcome bacterial resistance.Through a systematic investigation of the synthesis pathways,the efficiency of cephalosporin derivative synthesis and product quality under various reaction conditions,including reaction temperature,time,and the amount of material,were explored.The optimal synthesis conditions were identified as reaction temperature of 25℃,reaction time of 2 h,and 0.15 mol of 7-ACA.The antibacterial efficacy of the synthesized cephalosporin derivatives was evaluated through inhibition zone diameter testing and minimum inhibitory concentration(MIC)experiments,demonstrating significant antibacterial activity against Staphylococcus aureus and Escherichia coli.Although the antibacterial potency of these derivatives requires further enhancement compared to the existing antibiotics,they show considerable potential in expanding the antibacterial spectrum and overcoming bacterial resistance.The structure of the synthesized product was characterized,and its molecular formula can be deduced as C_(17)H_(19)N_(5)O_(5)S.
作者
董永广
DONG Yong-guang(Hebei Jiheng Pharmaceutical Co.,Ltd.,Hengshui 053000,China)
出处
《精细化工中间体》
CAS
2024年第5期19-24,共6页
Fine Chemical Intermediates
关键词
头孢哌酮衍生物
抗菌活性
合成路径
cephalosporin derivatives
antibacterial activity
synthetic pathways
