A General Approach to the Synthesis of Polyamine Linked-Monoindolylmaleimides, a New Series of Trypanothione Reductase Inhibitors

Abstract

A simplified approach to the synthesis of 2-polyamine linked-monoindolylmaleimides has been achieved, leading to a new series of trypanothione reductase inhibitors. The conditions of access to N, 2-bis(polyamine)-3-monoindolylmaleimides and N, N'-bis(monoindolylmaleimide) polyamines are described. Measured inhibitory activities towards trypanothione reductase from Tryanosoma cruzi show the importance of both aromatic moieties and polyamine chains for trypanothione reductase recognition.