Synthesis and structure− activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei …

DC Greenbaum, Z Mackey, E Hansell… - Journal of medicinal …, 2004 - ACS Publications
DC Greenbaum, Z Mackey, E Hansell, P Doyle, J Gut, CR Caffrey, J Lehrman, PJ Rosenthal
Journal of medicinal chemistry, 2004ACS Publications
We have synthesized a library of thiosemicarbazones and screened them against three
parasitic cysteine proteases, cruzain, falcipain-2, and rhodesain, and against the respective
parasite sources of these three proteases, Trypanosoma cruzi, Plasmodium falciparum, and
Trypanosoma brucei. The screens identified compounds that were effective against the
enzymes and the parasites but also some compounds that were parasiticidal despite a lack
of activity against the proteases. Several compounds were effective in killing all tested …
We have synthesized a library of thiosemicarbazones and screened them against three parasitic cysteine proteases, cruzain, falcipain-2, and rhodesain, and against the respective parasite sources of these three proteases, Trypanosoma cruzi, Plasmodium falciparum, and Trypanosoma brucei. The screens identified compounds that were effective against the enzymes and the parasites but also some compounds that were parasiticidal despite a lack of activity against the proteases. Several compounds were effective in killing all tested parasites. These promising lead compounds were tested for general toxicity in mice, and only one produced observable toxicity after 62 h. Our results suggest that thiosemicarbazones represent validated drug leads that kill several species of protozoan parasites through the inhibition of cysteine proteases as well as other novel targets.
ACS Publications
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