Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets

Citation
E. Davioud-charvet et al., Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets, BIOORG MED, 9(11), 1999, pp. 1567-1572
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
11
Year of publication
1999
Pages
1567 - 1572
Database
ISI
SICI code
0960-894X(19990607)9:11<1567:SOPDFT>2.0.ZU;2-8
Abstract
The most potent trypanocidal compound of a series of symmetrically substitu ted 1,4-bis(3-aminopropylpiperazines) which displayed an IC50 value of 5 mu M On Trypanosoma cruzi trypomastigotes, was inactive on trypanothione redu ctase. Two derivatives 6 and 12 of this compound, one symmetrical and one d issymmetrical, were synthesized via a reductive amination reaction, to prep are affinity chromatography columns, which allowed us to isolate three para sitic proteins. Among these, the major ligand 6- and 12-binding protein hav ing an apparent molecular weight of 52 kDa has been identified as the thiol -disulfide oxido-reductase Tc52, previously characterized in Trypanosoma cr uzi. (C) 1999 Elsevier Science Ltd. All rights reserved.