Synthesis and Biological Activity of Novel 3-(2-Propenyl)-Cephalosporins II. Preparation of Prodrugs

Abstract

Three prodrug esters (2a~2c) of 3-(2-propenyl)cephem (1a) have been prepared and their oral absorption was determined in rats and mice. While pivaloyloxymethyl ester (2a) did not improve the oral absorption of the parent cephem 1a, [(1-methyl)ethoxycarbonyloxy]ethyl ester (2b) and (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl ester (2c) improved oral absorption by a factor of five. © 1991, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.