Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 9, Pages 2883-2885Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.03.083
Keywords
sleeping sickness; HAT; African trypanosomiasis; cathepsins; TbCatB; rhodesain; thiosemicarbazone; protease inhibitors
Categories
Funding
- NCRR NIH HHS [P41 RR001614, P41 RR001614-246970] Funding Source: Medline
- NIAID NIH HHS [AI35707, P01 AI035707-05, P01 AI035707] Funding Source: Medline
Ask authors/readers for more resources
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 these compounds was determined against cultured T. brucei, and specificity was assessed with a panel of four mammalian cell lines. (c) 2008 Elsevier Ltd. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available