CAJ | 학술논문

目的设计、合成红霉素4"-氨基甲酸酯衍生物,研究其抗菌活性.方法以阿奇霉素为起始原料, 经1, 1'-羰基二咪唑处理以及胺解反应、曼尼希反应制备目标化合物, 并以金黄葡萄球菌为试验菌进行体外抗菌活性研究.结果共合成了9个目标化合物, 其结构经IR、13C NMR、 1H NMR和元素分析得以证实,经体外抗菌活性试验发现化合物 F-3 和 F-4 显示较好抗金黄色葡萄球菌活性,所有化合物无体外杀菌活性.结论说明吡咯烷基或哌啶基可能有利于提高抗菌活性.
목적 설계、합성홍매소4"-안기갑산지연생물,연구기항균활성.방법 이아기매소위기시원료, 경1, 1'-탄기이미서처리이급알해반응、만니희반응제비목표화합물, 병이금황포도구균위시험균진행체외항균활성연구.결과 공합성료9개목표화합물, 기결구경IR、13C NMR、 1H NMR화원소분석득이증실,경체외항균활성시험발현화합물 F-3 화 F-4 현시교호항금황색포도구균활성,소유화합물무체외살균활성.결론 설명필각완기혹고정기가능유리우제고항균활성.
Aim To synthesize 4"-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4"-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, 1H NMR and 13C NMR, and the synthetic condition (reagent ratios) was exploited. Among them, compounds F-3 and F-4 showed strong antibacterial activities against Staphylococcus aureus. But, all compounds did not show bactericidal activity. Discussion The test results showed that piperidinyl or pyrrolidinyl group may be of benefit to enhancing antibacterial activities.