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Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases |
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| Authors: | Miles Timothy J Barfoot Christopher Brooks Gerald Brown Pamela Chen Dongzhao Dabbs Steven Davies David T Downie David L Eyrisch Susanne Giordano Ilaria Gwynn Michael N Hennessy Alan Hoover Jennifer Huang Jianzhong Jones Graham Markwell Roger Rittenhouse Stephen Xiang Hong Pearson Neil |
| Affiliation: | aDiseases of the Developing World CEDD, GlaxoSmithKline, Calle Severo Ochoa, 2, 28760, Tres Cantos, Madrid, Spain;bInfectious Diseases CEDD, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, UK;cInfectious Diseases CEDD, GlaxoSmithKline, Third Avenue, Harlow CM19 5AW, UK;dInfectious Diseases CEDD, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;eBiological Reagents & Assay Development, GlaxoSmithKline, Gunnels Wood Road, Stevenage SG1 2NY, UK |
| Abstract: | As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoisomerases II and IV. We have investigated various subunits in this series and report advanced studies on compound 7 which demonstrates good PK and in vivo efficacy properties. |
| Keywords: | Antibacterials Bacterial type IIA topoisomerase Cyclohexyl-amides Pharmacokinetic In vivo efficacy |
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