Synthesis and biological activity of C-3' ortho dihydroxyphthalimido cephalosporins.
A series of C-3' ortho dihydroxyphthalimido cephalosporins 3-7 has been prepared by reaction of C-3' aminomethyl cephalosporin 41 with the corresponding N-carboethoxyphthalimides 23-25, 37, 38. These new cephalosporins exhibit excellent in vitro Gram-negative activities, including Pseudomonas aeruginosa, excellent beta-lactamases stability and pharmacokinetics equivalent or better than ceftriaxone.
Baudart
M G
MG
ZENECA pharma, Centre de Recherches Chemin de Vrilly, Reims, France.
Hennequin
L F
LF
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D002144:Callithrix; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D004355:Drug Stability; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D010797:Phthalimides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001618:beta-Lactamases / Q000378:metabolism
D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D010797:Phthalimides; D001618:beta-Lactamases