-
Bioorg. Med. Chem. Lett. · May 2008
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
- Jeremy P Mallari, Anang Shelat, Aaron Kosinski, Conor R Caffrey, Michele Connelly, Fangyi Zhu, James H McKerrow, and R Kiplin Guy.
- Graduate Program in Chemistry and Chemical Biology, University of California, San Francisco, CA 94143-2280, USA.
- Bioorg. Med. Chem. Lett. 2008 May 1; 18 (9): 2883-5.
AbstractHuman 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.
Notes
Knowledge, pearl, summary or comment to share?You can also include formatting, links, images and footnotes in your notes
- Simple formatting can be added to notes, such as
*italics*,_underline_or**bold**. - Superscript can be denoted by
<sup>text</sup>and subscript<sub>text</sub>. - Numbered or bulleted lists can be created using either numbered lines
1. 2. 3., hyphens-or asterisks*. - Links can be included with:
[my link to pubmed](http://pubmed.com) - Images can be included with:
 - For footnotes use
[^1](This is a footnote.)inline. - Or use an inline reference
[^1]to refer to a longer footnote elseweher in the document[^1]: This is a long footnote..