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ID: ALA1124865

Journal: J Med Chem

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

Authors: Brown RF, Kinnick MD, Morin JM, Vasileff RT, Counter FT, Davidson EO, Ensminger PW, Eudaly JA, Kasher JS, Katner AS.

Abstract: The preparation and biological evaluation of a series of 7 beta-[2-(2-aminothiazol-4-yl)-2(Z)-methoximinoacetamido]cep halosporins, 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, beta-lactamase stability, and in vitro and in vivo pharmacological evaluations are presented.

CiteXplore: 2115587

DOI: 10.1021/jm00170a011