Abstrakt: |
LY163892 is a new orally absorbed carbacephem. It inhibited and at ≤1 mg/l, but was less active against group B streptococci and groups C, F, G and bovis streptococci with MICs of 1 to 2 mg/l for most but as high as 8 mg/l for some isolates. MIC of methicillin-susceptible was 8 mg/l, but >128 mg/l for methicillin-resistant staphylococci. LY163892 had activity similar to cefaclor and cephalexin with MIC values of 16 mg/l for , 8 mg/l for , but was more active against , and . It had no activity against , and and spp. LY163892 was more rapidly lytic than cephalexin. It was hydrolyzed by a number of plasmid and chromosomal β-lactamases. For TEM-l, the = 354.7 μM, 25 = 2.5 μMoles/min/mg of protein, P99 = 24.3 μM, =28.9 μM/min/ug of protein, PC = 47.4 μM, = 2.7 μMoles/min/mg of protein. Overall it had β-lactamase stability similar to cefaclor, less than cephalexin, and markedly less than cefuroxime. [ABSTRACT FROM PUBLISHER] |