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.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry*
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Amides / pharmacokinetics
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Animals
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry*
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Anti-Bacterial Agents / pharmacology*
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Binding Sites
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Computer Simulation
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DNA Topoisomerases, Type II / chemistry*
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DNA Topoisomerases, Type II / metabolism
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Dogs
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Gram-Negative Bacteria / drug effects*
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Gram-Positive Bacteria / drug effects*
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Haplorhini
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Humans
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Microbial Sensitivity Tests
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Protein Structure, Tertiary
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Rats
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Structure-Activity Relationship
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Topoisomerase II Inhibitors / chemical synthesis
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Topoisomerase II Inhibitors / chemistry*
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Topoisomerase II Inhibitors / pharmacokinetics
Substances
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Amides
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Anti-Bacterial Agents
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Topoisomerase II Inhibitors
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DNA Topoisomerases, Type II