Orally active 2-(alkyloxycarbonyl)-2-alkylideneethyl esters of cephalosporins.

J Antibiot (Tokyo)

Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., Basel, Switzerland.

Published: August 1992

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.

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http://dx.doi.org/10.7164/antibiotics.45.1358DOI Listing

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