Grepafloxacin, a Dimethyl Derivative of Ciprofloxacin, Acts Preferentially through Gyrase in Streptococcus pneumoniae : Role of the C-5 Group in Target Specificity
Open Access
- 1 February 2002
- journal article
- research article
- Published by American Society for Microbiology in Antimicrobial Agents and Chemotherapy
- Vol. 46 (2) , 582-585
- https://doi.org/10.1128/aac.46.2.582-585.2002
Abstract
Grepafloxacin, a 5- methyl -7-piperazinyl-3"- methyl analogue of ciprofloxacin, was used to obtain stepwise-selected mutants of Streptococcus pneumoniae 7785. Analysis of the quinolone resistance-determining regions of the gyrA , gyrB , parC , and parE genes in these mutants revealed that gyrA mutations preceded those in parC . Given that ciprofloxacin (5- H ,7-piperazinyl) and AM-1121 (5- H ,7-piperazinyl-3"- methyl ) both act through topoisomerase IV, we conclude that the 5- methyl group of grepafloxacin favors gyrase in S. pneumoniae .Keywords
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