【摘要】 以6,8-二取代香豆素-13-羧酸为侧链酸,用酰氯法与7-ADCA、7-ACA、7-ACT、7-ACD缩合,合成了15个6,8-二取代香豆素-3-甲酰胺头孢菌素衍生物（Ⅵ）。经葡聚糖凝胶Sephade LH20和离心薄层层析分离精制,得到纯品。初步的体外抑菌试验结果表明,化合物Ⅵ₄、Ⅵ₆、Ⅵ₈、Ⅵ₁₁、Ⅵ₁₅对金黄色葡萄球菌26003和八叠球菌有中度和中度以上的抑菌作用。更多还原

【Abstract】 A series of the cephalosporin derivatives were designed and prepared by means of the direct condensation of 6, 8-disubstituted coumarin-3-carboxylic acids and the 7-aminogroup of 7-ADCA, 7-ACA, 7-ACT or 7-ACD. Isolation and purification were then conducted with the combined method on sephadex LH-20 column chromato graphy and centrifagel-t. 1. c technique. Fifteen novel cephalosporin derivatives were synthesized.Most of these novel derivatives, particularly compounds Ⅵ₄, Ⅳ₆, Ⅳ₈, Ⅳ₁₁ and Ⅳ₁₅, exhibited certein sensitivities to gram-positive bacteria in antibacterial sensitivity tests. Bacteriostasis was also observed to some gram-negative bacteria.更多还原