title: New spermine and spermidine derivatives as potent inhibitors of Trypanosoma cruzi trypanothione reductase.
abstract: Several spermine and spermidine derivatives containing 2-amino diphenylsulfide substituents were prepared and tested for their inhibiting effects on Trypanosoma cruzi trypanothione reductase. IC50 values were assessed between 0.3 and 3 microM. Compound 32 (Ki = 0.4 microM) is the most potent TR inhibitor described so far.
authors.affiliation: Laboratoire de Chimie des Biomolécules, URA CNRS 1309, Institut Pasteur, Faculté de Pharmacie, Lille, France.
authors.forename: B
authors.initials: B
authors.lastname: Bonnet
authors.forename: D
authors.initials: D
authors.lastname: Soullez
authors.forename: E
authors.initials: E
authors.lastname: Davioud-Charvet
authors.forename: V
authors.initials: V
authors.lastname: Landry
authors.forename: D
authors.initials: D
authors.lastname: Horvath
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors*; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors*; D013095:Spermidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013096:Spermine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014349:Trypanosoma cruzi / Q000187:drug effects / Q000201:enzymology*
chemical_list: D004791:Enzyme Inhibitors; D015800:Protozoan Proteins; D013096:Spermine; D009247:NADH, NADPH Oxidoreductases; C049608:trypanothione reductase; D013095:Spermidine