Selective inhibition of trypanosomal glyceraldehyde-3-phosphate dehydrogenase by protein structure-based design: toward new drugs for the treatment of sleeping …

…, S Van Calenbergh, A Van Aerschot…

Index: Verlinde, Christophe L. M. J.; Callens, Mia; Calenbergh, Serge Van; Aerschot, Arthur Van; Herdewijn, Piet; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 21 p. 3605 - 3613

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Citation Number: 82

Abstract

Sleeping sickness is considered by the World Health Organization as one of the major tropical parasitic diseases. l It is caused by the protozoon Trypanosoma brucei and is always fatal if untreated. Current chemotherapy of sleeping sickness is unsatisfactory. Pentamidine and suramin are only useful in the early stages of the infecti0n. l Melarsoprol is used in late- stage disease but frequently leads to fatal side effects. 2 The recently introduced drug ...