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

Verissimo, Edite; Berry, Neil; Gibbons, Peter D.; Cristiano, Maria Lurdes Santos; Rosenthal, Philip J.; Gut, Jiri; Ward, Stephen A.; O'Neill, Paul M.

http://hdl.handle.net/10400.1/4221

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Authors

Verissimo, Edite

Berry, Neil

Gibbons, Peter D.

Cristiano, Maria Lurdes Santos

Abstract(s)

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.

Keywords

Malaria Plasmodium falciparum Cysteine protease Falcipain-2 Peptidomimetic

URI

http://hdl.handle.net/10400.1/4221

Citation

Verissimo, Edite; Berry, Neil; Gibbons, Peter; Cristiano, M. Lurdes S.; Rosenthal, Philip J.; Gut, Jiri; Ward, Stephen A.; O’Neill, Paul M. Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors, Bioorganic & Medicinal Chemistry Letters, 18, 14, 4210-4214, 2008.