Anti-trypanosomal compounds. I. In vivo and in vitro activity of inhibitors of glycolysis in trypanosomes

Abstract

Carboxylated and phosphorylated esters of glycerol, possible inhibitors of the atypical glycolysis in trypanosomes have been synthesised and tested on Trypanosoma equiperdum in vitro and Trypanosoma brucei, on mice, and some of them also on glycerol phosphate dehydrogenase (GDH). Two of these compounds which showed no in vitro activity behaved as good competitive inhibitors of GDH; 3 other compounds were shown to have a good activity on cultures of trypanosomes, but owing to their weak solubility, tests on the enzyme could not be conclusive. Indications for the design of other compounds have been given.