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)-methoximinoacetamido]cephalosporins, 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