Orally active 2-(alkyloxycarbonyl)-2-alkylideneethyl esters of cephalosporins.
2-(Alkyloxycarbonyl)-2-alkylideneethyl esters of various aminothiazole-oxyimino cephalosporins have been synthesized and studied. They are useful alternatives to the currently existing orally active esters. Among the new esters synthesized, the 3'-azidomethyl cephem ester Ro 41-3399 (7k) presented an oral bioavailability superior to the corresponding pivaloyloxymethyl ester (9) in a rat model and was selected as a candidate for further evaluation.
Hubschwerlen
C
C
Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Charnas
R
R
Angehrn
P
P
Furlenmeier
A
A
Graser
T
T
Montavon
M
M
D000284:Administration, Oral; D000818:Animals; D002511:Cephalosporins / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D004952:Esters / Q000493:pharmacokinetics; D007408:Intestinal Absorption; D051379:Mice; D013329:Structure-Activity Relationship
D002511:Cephalosporins; D004952:Esters