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

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 acti...

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Bibliographic Details
Main Author: Verissimo, Edite (author)
Other Authors: Berry, Neil (author), Gibbons, Peter D. (author), Cristiano, Maria Lurdes Santos (author), Rosenthal, Philip J. (author), Gut, Jiri (author), Ward, Stephen A. (author), O'Neill, Paul M. (author)
Format: article
Language:eng
Published: 2014
Subjects:
Malaria
Plasmodium falciparum
Cysteine protease
Falcipain-2
Peptidomimetic
Online Access:http://hdl.handle.net/10400.1/4221
Country:Portugal
Oai:oai:sapientia.ualg.pt:10400.1/4221
Description
Summary: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.

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