Preparation, anti-trypanosomal activity and localisation of a series of dipeptide-based vinyl sulfones

An improved, Weinreb amide-based, synthesis of anti-trypanosomal lysine-containing vinyl sulfones is described incorporating, as a feature, diversity at the epsilon-lysine amino group. Members of this family demonstrated moderate to good efficacy as anti-trypanosomal agents and a fluorescent dansyl...

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Bibliographic Details
Published inOrganic & biomolecular chemistry Vol. 12; no. 38; pp. 7561 - 7571
Main Authors Doherty, William, James, Jinju, Evans, Paul, Martin, Laura, Adler, Nikoletta, Nolan, Derek, Knox, Andrew
Format Journal Article
LanguageEnglish
Published CAMBRIDGE Royal Soc Chemistry 14.10.2014
Subjects
Biological Transport
Chemistry
Chemistry Techniques, Synthetic
Chemistry, Organic
Dipeptides - chemistry
Intracellular Space - metabolism
Physical Sciences
Science & Technology
Sulfones - chemical synthesis
Sulfones - chemistry
Sulfones - metabolism
Sulfones - pharmacology
Trypanocidal Agents - chemical synthesis
Trypanocidal Agents - chemistry
Trypanocidal Agents - metabolism
Trypanocidal Agents - pharmacology
Trypanosoma brucei brucei - drug effects
IMIDAZOLE-1-SULFONYL AZIDE
ORGANIC-SYNTHESIS
DESIGN
TRYPANOSOMA-BRUCEI
CYSTEINE PROTEASE INHIBITORS
PARASITIC DISEASES
CHEMISTRY
INFECTION
DIAZOTRANSFER REAGENT
CHEMOTHERAPY
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Summary:An improved, Weinreb amide-based, synthesis of anti-trypanosomal lysine-containing vinyl sulfones is described incorporating, as a feature, diversity at the epsilon-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.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob01412j