Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain

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

文献索引：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

全文：HTML全文

被引用次数: 136

摘要

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 ...