SUBSTANCES AND PHARMACEUTICAL COMPOSITIONS FOR THE INHIBITION OF GLYOXALASES AND THEIR USE AGAINST PROTOZOA AND HELMINTHES

摘要

The present invention pertains to substances of the formula (I) wherein X is O or S; and R1 is a branched or non-branched alkyl, cycloalkyl, branched or non-branched alkenyl, cycloalkenyl, branched or non-branched alkinyl, cycloalkinyl, alkoxyalkyl, alkoxycarbonylalkyl, aryl or a sugar residue; and R2 is H or a branched or non-branched alkyl, cycloalkyl, branched or non-branched alkenyl, cycloalkenyl, branched or non-branched alkinyl, cycloalkinyl, alkoxyalkyl, alkoxycarbonylalkyl or aryl residue; and R3 and R4 together are =O, or R3 is OH and R4 is H; or R3 is H and R4 is OH. The invention relates to compounds of the general formula (I) for the inhibition of glyoxalase I and/or II, pharmaceutical compositions comprising one or more compounds according to formula (I), the use of one or more compounds according to formula (I) for the preparation of a medicament, and methods of treatment comprising the administration of one or more compounds according to formula (I). In particular, the present invention relates to the effects of a substance of formula (I) against parasites selected from protozoa and helminthes. The compound of formula (I), pharmaceutical composition, medicament or method of treatment related to said compound of the invention are for the treatment of diseases associated with increased glycolytic metabolism, comprising diseases associated with one or more of: increased formation of methylglyoxal, increased activity of glyoxalase I and/or II activity, and enhanced cell growth/proliferation. In one embodiment, the disease is a parasitic disease, wherein the parasite is selected from protozoa and helminthes.