title: Preparation, anti-trypanosomal activity and localisation of a series of dipeptide-based vinyl sulfones.
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.
authors.affiliation: Centre for Synthesis and Chemical Biology, School of Chemistry and Chemical Biology, University College Dublin, Dublin 4, Ireland. paul.evans@ucd.ie.
authors.forename: William
authors.initials: W
authors.lastname: Doherty
authors.forename: Jinju
authors.initials: J
authors.lastname: James
authors.forename: Paul
authors.initials: P
authors.lastname: Evans
authors.forename: Laura
authors.initials: L
authors.lastname: Martin
authors.forename: Nikoletta
authors.initials: N
authors.lastname: Adler
authors.forename: Derek
authors.initials: D
authors.lastname: Nolan
authors.forename: Andrew
authors.initials: A
authors.lastname: Knox
mesh_terms: D001692:Biological Transport; D060326:Chemistry Techniques, Synthetic; D004151:Dipeptides / Q000737:chemistry*; D042541:Intracellular Space / Q000378:metabolism; D013450:Sulfones / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D004151:Dipeptides; D013450:Sulfones; D014344:Trypanocidal Agents; C009873:divinyl sulfone