STUDIES ON ORALLY ACTIVE CEPHALOSPORIN ESTERS

VI. SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 3-(3-ISOXAZOLYL)OXYMETHYL CEPHALOSPORIN DERIVATIVES

Abstract

The synthesis and biological activities of a series of 3-(isoxazol-3-yl)oxymethyl cephalosporins are described. 7-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido] -3- [ (isoxazol-3-yl)oxy- methyl]-3-cephem-4-carboxylic acid (7a) showed potent activity against both Gram-positive and Gram-negative bacteria including some β-lactamase producing species. Its pivaloyloxymethyl ester provided a good urinary recovery after oral administration to mice.