期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 22, 页码 5860-5863出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.06.012
关键词
Cysteine protease inhibitors; Macrocyclic dipeptidyl vinyl sulfones
资金
- National Institutes of Allergy and Infectious Diseases [AI 35707]
The importance of cysteine proteases in parasites, compounded with the lack of redundancy compared to their mammalian hosts makes proteases attractive targets for the development of new therapeutic agents. The binding mode of K11002 to cruzain, the major cysteine protease of Trypanosoma cruzi was used in the design of conformationally constrained inhibitors. Vinyl sulfone-containing macrocycles were synthesized via olefin ring-closing metathesis and evaluated against cruzain and the closely related cysteine protease, rhodesain. (C) 2008 Elsevier Ltd. All rights reserved.
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