【摘要】 以阿奇霉素11,12-环硼酸酯为原料,设计并合成了18个阿奇霉素4’’-取代亚苄肼基甲酸酯及4’’-取代亚苄肼基甲酸酯-11,12-环碳酸酯衍生物。体外抗菌活性试验结果表明,所得化合物对受试革兰阳性菌如金黄色葡萄球菌、表皮葡萄球菌、白色葡萄球菌和肺炎双球菌抗菌活性良好,部分化合物对丙型链球菌、革兰阴性菌如鲍氏志贺氏菌和普通变形杆菌也有较强的抗菌活性。更多还原

【Abstract】 Eighteen new azithromycin 4’’-substituted benzal hydrazinoformate and 4’’-substituted benzal hydrazinoformate-11,12-cyclic carbonate derivatives were synthesized from azithromycin 11,12-cyclic borate.The antibacterial activity of the title compounds was evaluated in vitro and the results showed that these compounds exhibited good antibacterial activity against tested gram-positive bacteria,such as Staphylococcus aureus,Staphylococcus epidermidis,Staphylococcus albus,and Diplococcus lanceolatus.Some of the compounds were also very active against Gamma streptococcus,gram-negative strains including Shigella boydii and Proteus vulgaris.更多还原