Studies on orally active cephalosporin esters.
The synthesis and the biological properties of orally active cephalosporin esters are described. 3-Methoxymethyl cephem derivatives having a 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamide function at C-7 (1) showed good activity against a wide variety of bacteria including some beta-lactamase producing species. The prodrug type esters of 1 exhibited a good urinary recovery after oral administration to mice and 1-(isopropoxycarbonyloxy)ethyl ester (2a, CS-807) has been pre-clinically tested as an orally active cephem prodrug.
D000284:Administration, Oral; D000818:Animals; D001424:Bacterial Infections / Q000188:drug therapy; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D004952:Esters; D051379:Mice; D051381:Rats
D002511:Cephalosporins; D004952:Esters