Published in
Elsevier, Bioorganic and Medicinal Chemistry Letters, 14(18), p. 4210-4214
DOI: 10.1016/j.bmcl.2008.05.068
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Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors
Journal article published in 2008 by
Edite Verissimo,
Neil Berry,
Peter Gibbons,
M. Lurdes S. Cristiano 
,
Philip J. Rosenthal,
Jiri Gut,
Stephen A. Ward,
Paul M. O'Neill
,
Philip J. Rosenthal,
Jiri Gut,
Stephen A. Ward,
Paul M. O'Neill
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Abstract
The structure-based design, chemical synthesis and in vitro activity evaluation of various falcipain inhibitors derived from 2-pyridone are reported. These compounds contain a peptidomimetic binding determinant and a Michael acceptor terminal moiety capable of deactivating the cysteine protease active site. (C) 2008 Elsevier Ltd. All rights reserved.