Synthesis and biological evaluation of glutathione-like tripeptidesagainstTrypanosoma cruzi

Abstract

Glutathionylspermidine synthase (GSS) is a crucial enzyme in the trypanothione biosynthetic pathway and is also an interesting molecular target for drug design. We synthesized a series of amides of a glutathione analogue (L-γ-Glu-L-Leu-Gly-NHR) where R are linear alkyl groups. All of these drugs exhibited marginal biological activity against the responsible agent of Chagas' disease, the protozoan Trypanosoma cruzi.