A GENERAL-APPROACH TO THE SYNTHESIS OF POLYAMINE LINKED-MONOINDOLYLMALEIMIDES, A NEW SERIES OF TRYPANOTHIONE REDUCTASE INHIBITORS

Citation
L. Salmon et al., A GENERAL-APPROACH TO THE SYNTHESIS OF POLYAMINE LINKED-MONOINDOLYLMALEIMIDES, A NEW SERIES OF TRYPANOTHIONE REDUCTASE INHIBITORS, Chemical and Pharmaceutical Bulletin, 46(4), 1998, pp. 707-710
Citations number
24
Categorie Soggetti
Chemistry Medicinal",Chemistry,"Pharmacology & Pharmacy
ISSN journal
00092363
Volume
46
Issue
4
Year of publication
1998
Pages
707 - 710
Database
ISI
SICI code
0009-2363(1998)46:4<707:AGTTSO>2.0.ZU;2-7
Abstract
A simplified approach to the synthesis of 2-polyamine linked-monoindol ylmaleimides has been achieved, leading to a new series of trypanothio ne reductase inhibitors. The conditions of access to N,2-bis(polyamine )-3-monoindolylmaleimides and N,N'-bis(monoindolylmaleimide) polyamine s are described. Measured inhibitory activities towards trypanothione reductase from Tryanosoma cruzi show the importance of both aromatic m oieties and polyamine chains for trypanothione reductase recognition.