Synthesis and biological evaluation of a series of parenteral 3'-quaternary ammonium cephalosporins

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Abstract
The preparation and biological evaluation of a series of 7.beta.-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cephalosporins, substituted at the 3''-position with monocyclic or bicycle 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, .beta.-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented.