Mechanism of action of the des-F(6) quinolone BMS-284756 measured by supercoiling inhibition and cleavable complex assays

P Wu; L E Lawrence; K L Denbleyker; J F Barrett

doi:10.1128/AAC.45.12.3660-3662.2001

Mechanism of action of the des-F(6) quinolone BMS-284756 measured by supercoiling inhibition and cleavable complex assays

Antimicrob Agents Chemother. 2001 Dec;45(12):3660-2. doi: 10.1128/AAC.45.12.3660-3662.2001.

Authors

P Wu¹, L E Lawrence, K L Denbleyker, J F Barrett

Affiliation

¹ Bristol-Myers Squibb Company Pharmaceutical Research Institute, Wallingford, Connecticut, USA.

Abstract

BMS-284756 (T-3811ME), a novel des-F(6) quinolone, was tested in the supercoiling inhibition and cleavable complex assays against Escherichia coli DNA gyrase, a target of quinolones. The results suggest that BMS-284756 has the same mechanism of action against DNA gyrase as other quinolones and a similar level of potency.

MeSH terms

Anti-Infective Agents / pharmacology*
DNA, Bacterial / drug effects*
DNA, Superhelical / drug effects*
Enzyme Inhibitors / pharmacology*
Escherichia coli / drug effects
Escherichia coli / enzymology*
Fluoroquinolones*
Gram-Negative Bacteria / drug effects
Gram-Positive Bacteria / drug effects
Indoles*
Microbial Sensitivity Tests
Quinolones*
Topoisomerase II Inhibitors*

Substances

Anti-Infective Agents
DNA, Bacterial
DNA, Superhelical
Enzyme Inhibitors
Fluoroquinolones
Indoles
Quinolones
Topoisomerase II Inhibitors
garenoxacin