SYNTHESIS AND BIOLOGICAL EVALUATION OF A SERIES OF PARENTERAL 3'-QUATERNARY AMMONIUM CEPHALOSPORINS

The preparation and biological evaluation of a series of 7β-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacet-amidojcephalosporins, substituted at the 3’-position with monocyclic or bicyclic nitrogen-containing heterocycles are described. The resulting family of parenteral compounds displays a broad spectrum of antibacterial activity. Some compounds exhibit a similar level of Gram-negative activity to that of the “third-generation” cephalosporins with increased staphylococcal activity.The in vitro and in vivo antimicrobial activity, structure-activity relationships, β-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented. © 1990, American Chemical Society. All rights reserved.