.BETA.-Lactamase inhibitory activities and synergistic effects of 5,6-cis-carbapenem antibiotics.

Abstract
Twelve 5,6-cis-carbapenem antibiotics were examined for their .beta.-lactamase inhibitory activities, their types of inhibitions and their synergistic activities with other .beta.-lactam antibiotics. All the carbapenems inhibited 8 types of .beta.-lactamases including cephalosporinases which were insensitive to clavulanic acid and sulbactam. The sulfonyloxy ethyl carbapenems were the most active inhibitors; they inhibited all .beta.-lactamases in a progressive fashion, whereas some of the hydroxyl compounds exerted non-progressive inhibition against several .beta.-lactamases, such as those of Escherichia coli TN713 and Proteus vulgaris GH4413. Several carbapenems were inactivated by the .beta.-lactamases of Citrobacter freundii GN1706, P. vulgaris GN4413, E. coli TN713 and Klebsiella pneumoniae TN1698. Most of the carbapenems potentiated the antibacterial activities of ampicillin and cefotiam against .beta.-lactamase-producing bacteria.

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