Abstract
A series of inhibitors of the enzyme trypanothione reductase has been identified using directed solid-phase chemistry. The compounds were based on a series of polyamine scaffolds and used the natural product kukoamine A as the lead structure. A compound with a Ki of 76 nM was identified, although somewhat surprisingly the compound appeared to be noncompetitive in nature.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Drug Design
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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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Glutathione Reductase / antagonists & inhibitors
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Kinetics
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Molecular Structure
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NADH, NADPH Oxidoreductases / antagonists & inhibitors*
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Polyamines / chemical synthesis*
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Polyamines / chemistry
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Polyamines / pharmacology
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Structure-Activity Relationship
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Trypanocidal Agents / chemical synthesis*
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Trypanocidal Agents / chemistry
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Trypanocidal Agents / pharmacology
Substances
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Enzyme Inhibitors
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Polyamines
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Trypanocidal Agents
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NADH, NADPH Oxidoreductases
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trypanothione reductase
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Glutathione Reductase