阿奇霉素衍生物的合成和抗菌活性研究.Ⅲ.4″-取代亚乙基肼基甲酸酯

Synthesis and Antibacterial Activity of Azithromycin Derivatives.Ⅲ.4″-Substituted Ethylidene Hydrazinoformate

以阿奇霉素11,12-环硼酸酯为原料,设计并合成了17个阿奇霉素4″-取代亚乙基肼基甲酸酯及4″-取代亚乙基肼基甲酸酯-11,12-环碳酸酯衍生物。体外抗菌活性试验结果表明,目标化合物对受试表皮葡萄球菌、白色葡萄球菌、肺炎双球菌和丙型链球菌等革兰阳性菌,以及福氏志贺菌等革兰阴性菌抗菌活性良好,部分化合物对革兰阳性金黄色葡萄球菌和肠球菌也有较强的抗菌活性。

Seventeen new azithromycin 4＂-substituted ethylidene hydrazinoformate and 4＂-substituted ethylidene hydrazinoformate-11,12-cyclic carbonate derivatives were synthesized from azithromycin 11,12-cyclic borate. The antibacterial activity of the title compounds was tested in vitro and the results showed that these compounds exhibited good antibacterial activity against tested gram-positive bacteria, such as Staphylococcus epidermidis, Staphylococcus albus, Diplococcus lanceolatus, Gamma streptococcus and gram-negative Shigellaflexneri. Some of the compounds were also rather active against gram-positive Staphylococcus aureus and Enterococcus.