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: https://orcid.org/0000-0003-2331-3192 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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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.

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):	https://doi.org/10.1016/j.bmcl.2008.05.068
Depositing User:	Mary Creegan
Date Deposited:	24 Jun 2010 15:39
Last Modified:	06 Feb 2018 13:00
URI:	https://archive.lstmed.ac.uk/id/eprint/655

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