Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB

…, A Shelat, A Kosinski, CR Caffrey, M Connelly…

文献索引：Mallari, Jeremy P.; Shelat, Anang; Kosinski, Aaron; Caffrey, Conor R.; Connelly, Michele; Zhu, Fangyi; McKerrow, James H.; Guy, R. Kiplin Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 9 p. 2883 - 2885

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被引用次数: 53

摘要

Human African trypanosomiasis (HAT) is caused by the protozoan parasite Trypanosoma brucei. The cysteine proteases of T. brucei have been shown to be crucial for parasite replication and represent an attractive point for therapeutic intervention. Herein we describe the synthesis of a series of thiosemicarbazones and their activity against the trypanosomal cathepsins TbcatB and rhodesain, as well as human cathepsins L and B. The activity of ...