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

…, P Doyle, J Gut, CR Caffrey, J Lehrman…

Index: Greenbaum, Doron C.; Mackey, Zachary; Hansell, Elizabeth; Doyle, Patricia; Gut, Jiri; Caffrey, Conor R.; Lehrman, Julia; Rosenthal, Philip J.; McKerrow, James H.; Chibale, Kelly Journal of Medicinal Chemistry, 2004 , vol. 47, # 12 p. 3212 - 3219

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Citation Number: 216

Abstract

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 ...