Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 21, Pages 6218-6221Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.098
Keywords
Protease inhibitors; Cruzain; Rhodesain; Vinylsulfone
Categories
Funding
- Sandler Foundation
- Department of Energy
- Office of Biological and Environmental Research
- National Institutes of Health
- National Center for Research Resources
- National Institute of General Medical Sciences
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We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 angstrom) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such analogs bind the S2 and S3 subsites of the protease, effectively recapitulating important binding interactions present in more traditional peptide-based protease inhibitors and natural substrates. (c) 2009 Elsevier Ltd. All rights reserved.
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