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

Journal Article

TitleDesign and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors.
Publication TypeJournal Article
AuthorsVerissimo, E, Berry, N, Gibbons, P, Cristiano, MLS, Rosenthal, PJ, Gut, J, Ward, SA, O'Neill, PM
Year of Publication2008
JournalBioorg Med Chem Lett
Volume18
Issue14
Date Published2008 Jul 15
Pagination4210-4
ISSN1464-3405
KeywordsAnimals, Antimalarials, Chemistry, Pharmaceutical, Cysteine Endopeptidases, Cysteine Proteinase Inhibitors, Drug Design, Humans, Inhibitory Concentration 50, Malaria, Models, Chemical, Molecular Conformation, Plasmodium falciparum, Pyridones, Structure-Activity Relationship
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.
DOI10.1016/j.bmcl.2008.05.068
Sapientia

http://www.ncbi.nlm.nih.gov/pubmed/18554905?dopt=Abstract
Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID18554905
Grant ListBB/C006321/1 / / Biotechnology and Biological Sciences Research Council / United Kingdom
CCMAR Authors
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