Abstract

Moxalactam, a new synthetic β-lactam antibiotic, was evaluated for in vitro and in vivo antibacterial activity and was found to have a broad spectrum of activity against gram-positive and gram-negative bacteria. Moxalactam showed more potent activity than did' the cephalosporins tested against clinical gram-negative isolates, including cefazolin-resistant Enterobacteriaceae, glucose-nonfermenting bacteria, and Bacteroides fragilis. Moxalactam was the only β-lactam antibiotic of those tested (including nine penicillins and 15 cephalosporins) that was not affected by β-lactamase produced by 15 strains of 10 gram-negative species. The potent in vitro activity and high stability to β-Iactamase of moxalactam corresponded to lower ED50 (50% effective doses) required against intraperitoneal infections in mice due to various bacteria resistant to cefazolin, cefoxitin, or cefotiam. Furthermore, moxalactam showed the greatest therapeutic activity among the nine β-Iactam antibiotics tested in models of intraperitoneal mixed infection in mice with Escherichia coli and Pseudomonas aeruginosa.

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