Abstract
Ceftibuten is an oral third-generation cephalosporin active against a wide range of bacteria and shows an improved stability to hydrolysis by several ß-lactamases because of the carboxyethilidine moiety at position 7 of the ß-acyl side chain. The kinetic interactions between ceftibuten and active-site serine and metallo-ß-lactamases were investigated. The activity of several TEM-derived extended spectrum ß-lactamases (ESßLs) against ceftibuten, cefotaxime and ceftazidime was compared using K m, K cat and K cat/ K m. Ceftibuten behaved as a poor substrate for class A and B ß-lactamases compared with cefotaxime. The chromosomal class C ß-lactamase from Enterobacter cloacae 908R gave a high K cat value (21 s −1), whereas there was poor activity with enzymes from Acinetobacter baumannii and Morganella morganii and ceftibuten. Ceftibuten resists hydrolysis in the presence of typical respiratory or urogenital-tract pathogens producing ß-lactamases.
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