
Bioorganic and Medicinal Chemistry Letters p. 1567 - 1572 (1999)
Update date:2022-08-03
Topics:
Davioud-Charvet, Elisabeth
Berecibar, Amaya
Girault, Sophie
Landry, Valerie
Drobecq, Herve
Sergheraert, Christian
The most potent trypanocidal compound of a series of symmetrically substituted 1,4-bis(3-aminopropylpiperazines) which displayed an IC50 value of 5 μM on Trypanosoma cruzi trypomastigotes, was inactive on trypanothione reductase. Two derivatives 6 and 12 of this compound, one symmetrical and one dissymetrical, were synthesized via a reductive amination reaction, to prepare affinity chromatography columns, which allowed us to isolate three parasitic proteins. Among these, the major ligand 6- and 12-binding protein having an apparent molecular weight of 52 kDa has been identified as the thiol-disulfide oxido-reductase Tc52, previously characterized in Trypanosoma cruzi.
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