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

Verissimo, E., Berry, N., Gibbons, P., Cristiano, M. L. S., Rosenthal, P. J., Gut, J., Ward, Stephen ORCID: and O'Neill, P. M. (2008) 'Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors'. Bioorganic & Medicinal Chemistry Letters, Vol 18, Issue 14, pp. 4210-4214.

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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.

Item Type: Article
Uncontrolled Keywords: malaria plasmodium falciparum cysteine protease falcipain-2 peptidomimetic cysteine protease inhibitors plasmodium-falciparum biological evaluation proteinase malaria
Subjects: QU Biochemistry > Biochemistry of the Human Body > QU 100 Body composition
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
QX Parasitology > Protozoa > QX 135 Plasmodia
Faculty: Department: Groups (2002 - 2012) > Molecular & Biochemical Parasitology Group
Digital Object Identifer (DOI):
Depositing User: Mary Creegan
Date Deposited: 24 Jun 2010 15:39
Last Modified: 06 Feb 2018 13:00


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