Abstract
An improved, Weinreb amide-based, synthesis of anti-trypanosomal lysine-containing vinyl sulfones is described incorporating, as a feature, diversity at the ε-lysine amino group. Members of this family demonstrated moderate to good efficacy as anti-trypanosomal agents and a fluorescent dansyl (19) derivative was used to investigate subcellular localisation of the compound class.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Biological Transport
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Chemistry Techniques, Synthetic
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Dipeptides / chemistry*
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Intracellular Space / metabolism
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Sulfones / chemical synthesis
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Sulfones / chemistry*
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Sulfones / metabolism
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Sulfones / pharmacology*
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Trypanocidal Agents / chemical synthesis
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Trypanocidal Agents / chemistry*
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Trypanocidal Agents / metabolism
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Trypanocidal Agents / pharmacology*
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Trypanosoma brucei brucei / drug effects*
Substances
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Dipeptides
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Sulfones
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Trypanocidal Agents
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divinyl sulfone