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) presen...

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Veröffentlicht in:	Journal of antibiotics 1992/08/25, Vol.45(8), pp.1358-1364
Hauptverfasser:	HUBSCHWERLEN, CHRISTIAN, CHARNAS, ROBERT, ANGEHRN, PETER, FURLENMEIER, ANDREAS, GRASER, THEODOR, MONTAVON, MARC
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Cephalosporins - administration & dosage Cephalosporins - chemical synthesis Cephalosporins - pharmacokinetics Esters - pharmacokinetics Intestinal Absorption Medical sciences Mice Pharmacology. Drug treatments Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.45.1358