Ceftizoxime and other third-generation cephalosporins: structure-activity relationships

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Abstract
The aminothiazolyloximino cephalosporins are a major subgroup of analogues within the third-generation class of cephalosporins. The structure-activity relationship data presented demonstrate for these analogues that: (1) the α-oximino moiety imparts a high degree of stability to β-lactamases, (2) potency in vitro is strongly influenced by the configuration of the oxime—the syn isomer being the more active, (3) a methyl group attached to the oxime provides an optimum balance of Gram-positive and Gram-negative activities in vitro , though a bulky acidic function on the oxime can enhance activity against Ps. aeruginosa , and (4) incorporation of acidic character into a heterocyclic substituent attached to the 3-position of the cephalosporin nucleus can markedly increase peak serum levels and prolong serum half lives, a result which parallels earlier findings with other analogues.

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