New spermine and spermidine derivatives as potent inhibitors of Trypanosoma cruzi trypanothione reductase.
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.
Bonnet
B
B
Laboratoire de Chimie des Biomolécules, URA CNRS 1309, Institut Pasteur, Faculté de Pharmacie, Lille, France.
Soullez
D
D
Davioud-Charvet
E
E
Landry
V
V
Horvath
D
D
Sergheraert
C
C
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*
D004791:Enzyme Inhibitors; D015800:Protozoan Proteins; D013096:Spermine; D009247:NADH, NADPH Oxidoreductases; C049608:trypanothione reductase; D013095:Spermidine