STRUCTURE-ACTIVITY-RELATIONSHIPS IN 2-AMINODIPHENYLSULFIDES AGAINST TRYPANOTHIONE REDUCTASE FROM TRYPANOSOMA-CRUZI

Authors
GIRAULT S DAVIOUDCHARVET E SALMON L BERECIBAR A DEBREU MA SERGHERAERT C
Citation
S. Girault et al., STRUCTURE-ACTIVITY-RELATIONSHIPS IN 2-AMINODIPHENYLSULFIDES AGAINST TRYPANOTHIONE REDUCTASE FROM TRYPANOSOMA-CRUZI, Bioorganic & medicinal chemistry letters, 8(10), 1998, pp. 1175-1180
Citations number
22
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
10
Year of publication
1998
Pages
1175 - 1180
Database
ISI
SICI code
0960-894X(1998)8:10<1175:SI2AT>2.0.ZU;2-1
Abstract
In order to establish structural elements responsible for inhibition o f trypanothione reductase (TR) from Trypanosoma cruzi by 2-aminodiphen ylsulfides, a series of dissymmetrical derivatives, corresponding to t he replacement of one aromatic moiety by different amines, was synthes ized. TR inhibition studies revealed the importance of the aromatic ri ngs and of the amino groups in the side chains for potent inhibition. Quinonic moities were also introduced with the aim of acting as TR red ox-cycling substrates. (C) 1998 Elsevier Science Ltd. All rights reser ved.