
Bioorganic and Medicinal Chemistry Letters p. 1175 - 1180 (1998)
Update date:2022-09-26
Topics:
Girault, Sophie
Davioud-Charvet, Elisabeth
Salmon, Laurence
Berecibar, Amaya
Debreu, Marie-Ange
Sergheraert, Christian
In order to establish structural elements responsible for inhibition of trypanothione reductase (TR) from TrypanosoMa cruzi by 2- aminodiphenylsulfides, a series of dissymmetrical derivatives, corresponding to the replacement of one aromatic moiety by different amines, was synthesized. TR inhibition studies revealed the importance of the aromatic rings and of the amino groups in the side chains for potent inhibition. Quinonic moities were also introduced with the aim of acting as TR redox- cycling substrates.
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