FK 482, a new orally active cephalosporin. Synthesis and biological properties.

Abstract

Recently, we have reported the synthesis and biological properties of a new orally absorbable cephem, cefixime (CFIX, la) and the related compounds1~4). CFIX is the first orally active cephem having an aminothiazolyl side chain in the 7-position like newer parenteral cephalosporins such as ceftizoxime and has a broad spectrum of antibacterial activity and a high stability against various /3-lactamases. However, CFIX shows only low to moderate antibacterial activity against a few Gram-positive bacteria such as Staphylococcus aureus and Enterococcus faecalis. In the course of our