4.5 Article

Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 24, Pages 7483-7488

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.09.114

Keywords

Antibacterials; Bacterial type IIA topoisomerase; Cyclohexyl-amides; Pharmacokinetic; In vivo efficacy

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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. (C) 2011 Elsevier Ltd. All rights reserved.

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