Synthesis and biological activity of C-3' ortho dihydroxyphthalimido cephalosporins.
作者:MARIE-GENEVIÉVE BAUDART、LAURENT F. HENNEQUIN
DOI:10.7164/antibiotics.46.1458
日期:——
A series of C-3' ortho dihydroxyphthalimido cephalosporins 3-7 has been prepared by reaction of C-3' aminomethyl cephalosporin 411). with the corresponding N-carboethoxyphthalimides 23-25, 37, 38. These new caphalosporins exhibit excellent in vitro Gram-negative activities, including Pseudomonas aeruginosa, excellent β-lactamases stability and pharmacokinetics equivalent or better than ceftriaxone.
一系列C-3'邻二羟基酞酰亚胺甲基头孢菌素3-7通过C-3'氨基甲基头孢菌素411与相应的N-羰乙氧基酞酰亚胺23-25、37、38反应制备而成。这些新型头孢菌素显示出卓越的体外革兰氏阴性菌活性,包括铜绿假单胞菌,卓越的β-内酰胺酶稳定性,以及与头孢曲松相当或更优的药代动力学特性。