新型第4代头孢菌素类化合物的合成及抗菌活性
Synthesis and antibacterial activity of novel fourth-generation cephalosporin compounds
-
摘要: 目的 ： 研究新型第4代头孢菌素类化合物的合成及其抗菌活性。 方法 ： 7-氨基头孢霉烷酸(7-ACA)在三甲基碘硅烷(TMSI)催化下与含N芳杂环化合物进行3-位取代反应，再与盐酸反应转化为盐酸盐，最后在三乙胺催化下与2-(2-取代氨基噻唑-4-基)-(Z)-2-甲氧亚氨乙酸苯并噻唑硫醇活性酯缩合得到目标化合物，并通过平皿二倍稀释法对它们的体外抗菌活性进行评价。 结果和结论 ： 合成的9个目标化合物 4a~4i 均未见文献报道，其结构经IR、ESI-MS、1H NMR和元素分析确证。初步体外抗菌活性实验结果表明，化合物 4c和4h 对革兰氏阳性菌的活性与头孢唑兰相当。Abstract: Aim ：To study the synthesis and antibacterial activity of new fourth-generation cephalosporin compounds. Methods ：Starting with 7-ACA，the target compounds were obtained by 3-substitution with nitrogen-containing aromatic heterocyclic compounds using TMSI as a catalyst，salt exchange with hydrochloric acid and condensation with 2-(2-substituted aminothiazol-4-yl)-(Z)-2-methoxyiminoacetic acid thiobenzothiazole active esters in the presence of Et3N.Their antibacterial activity in vitro were evaluated by double broth dilution method. Results and Conclusion ：Nine new compounds were synthesized，and their structures were confirmed by IR，ESI-MS，1H NMR and elemental analysis.Preliminary results of antibacterial activities in vitro showed that compounds 4c and 4h possessed approximately equivalent antibacterial activity against Gram-positive bacteria in comparison with cefozopran.
-
Keywords:
- fourth-generation cephalosporins /
- synthesis /
- antibacterial activity
-
计量
- 文章访问数: 1183
- HTML全文浏览量: 1
- PDF下载量: 1601
下载:
