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
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.