Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain

…, EJ Hansell, Z Mackey, P Doyle, YM Zhou, J Gut…

Index: Fujii, Naoaki; Mallari, Jeremy P.; Hansell, Elizabeth J.; MacKey; Doyle, Patricia; Zhou; Gut, Jiri; Rosenthal, Philip J.; McKerrow, James H.; Guy, R. Kiplin Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 121 - 123

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Citation Number: 136

Abstract

Herein we report the synthesis and evaluation of a series of thiosemicarbazones as potential inhibitors of cysteine proteases relevant to parasitic diseases. Derivatives of thiosemicarbazone 1 were discovered to be potent inhibitors of cruzain and rhodesain, crucial proteases in the life cycles of Trypanosoma cruzi and T. brucei rhodesiense, the organisms causing Chagas' disease and sleeping sickness. However, the entire series ...