Abstract
We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3β inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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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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Dose-Response Relationship, Drug
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Escherichia coli / drug effects
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Glycogen Synthase Kinase 3 / antagonists & inhibitors*
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Glycogen Synthase Kinase 3 beta
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Microbial Sensitivity Tests
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Molecular Structure
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Nitriles / chemistry*
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Quinolizines / chemical synthesis
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Quinolizines / chemistry
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Quinolizines / pharmacology*
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Staphylococcus aureus / drug effects
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Enzyme Inhibitors
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Nitriles
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Quinolizines
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Glycogen Synthase Kinase 3 beta
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Glycogen Synthase Kinase 3