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Bioorg Med Chem Lett. 2008 Jul 15;18(14):4210-4. doi: 10.1016/j.bmcl.2008.05.068. Epub 2008 May 20.

Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors.

Author information

1
Department of Chemistry, Biochemistry and Pharmacy, and CCMAR, University of Algarve, Campus de Gambelas, Faro 8005-039, Portugal.

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.

PMID:
18554905
DOI:
10.1016/j.bmcl.2008.05.068
[Indexed for MEDLINE]

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