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Comparative in vitro activity of the new fluoroquinolone BMY-40062
Authors:N. X. Chin  H. Neu
Affiliation:(1) Department of Medicine, College of Physicians & Surgeons, Columbia University, 630 West 168 Street, 10032 New York, USA;(2) Department of Pharmacology, College of Physicians & Surgeons, Columbia University, 630 West 168 Street, 10032 New York, USA
Abstract:The results are presented of comparative in vitro susceptibility testing of BMY-40062, a new fluorinated quinolone which contains a tetrabutyl moiety at N-1 and a piperazinyl group at C-7. BMY-40062 inhibited 90 % ofEnterobacteriaceae strains at < 0.5 µg/ml, being either equal in activity to ciprofloxacin or two- to four-fold less active, depending upon the species. BMY-40062 was as active as ciprofloxacin againstPseudomonas aeruginosa (MIC90 0.5 µg/ml) and inhibited most other strains ofPseudomonas species at < 1 µg/ml. It was more active than ciprofloxacin or ofloxacin against hemolytic streptococci andStreptococcus pneumoniae, 90 % of strains being inhibited at < 0.5 µg/ml. MICs increased in the presence of 9 mM Mg2+ and at pH 5.5. The frequency of spontaneous mutation was low forEnterobacteriaceae, Pseudomonas aeruginosa andStaphylococcus aureus (10–10), but repeated exposure to BMY-40062 caused selection of resistant isolates. Clinical isolates ofPseudomonas aeruginosa resistant to ciprofloxacin and ofloxacin were resistant to BMY-40062.
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