Laboratory assessment of antibacterial activity of zwitterionic 7-methoxyimino cephalosporins.
Zwitterionic 7-methoxyimino cephalosporins (cefpirome, cefepime, cefclidin, DQ2556, FK037 and SCE2787) possess a variable substitution at C3 which contains a quarternary nitrogen. These cephalosporins display low affinities for Class I beta-lactamase and rapid penetration through the outer membrane of Gram-negative bacilli, so that an increased number of periplasmic beta-lactam molecules interact with PBP's per unit of time. As a consequence, the new zitterionic compounds remain active against some, but not all, ceftazidime-resistant Enterobacteriaceae producing high levels of Class I beta-lactamase or Bush type 2b beta-lactamases. Antipseudomonas activities are generally similar to that of ceftazidime except that cefclidin is more active. The new zwitterionic compounds, especially cefpirome and FK037, express greater antistaphylococcal potency than does ceftazidime. A variety of animal models including meningitis and endocarditis have confirmed the potential of these compounds in-vivo. On the basis of structural and antibacterial characteristics, the expression 'forth generation' is acceptable to describe the zwitterionic 7-methoxyimino cephalosporins.
Pechère
J C
JC
Department of Genetics and Microbiology, University of Geneva, Switzerland.
Wilson
W
W
Neu
H
H
D002511:Cephalosporins / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D002511:Cephalosporins