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2-Amino diphenylsulfides as inhibitors of trypanothione reductase: modification of the side chain.

Abstract：

:A molecular modeling study meant to detect pharmacophore-like patterns in the active site of trypanothione reductase (TR) offered hints about the opportunity of synthesizing and testing diphenylsulfide derivatives with prolonged or branched polyamino side chains as putative TR inhibitors. The inhibition results within the synthesized series confirmed the main working hypothesis inspired by the molecular modeling study. The different compounds were tested in vitro on the enzyme and on Trypanosoma cruzi and Trypanosoma brucei trypomastigotes as well as in vivo in infected mice.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Baillet S,Buisine E,Horvath D,Maes L,Bonnet B,Sergheraert C

doi

10.1016/0968-0896(96)00083-1

subject

Has Abstract

pub_date

1996-06-01 00:00:00

pages

891-9

issue

6

eissn

0968-0896

issn

1464-3391

pii

0968-0896(96)00083-1

journal_volume

4

pub_type

杂志文章

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