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

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Detalhes bibliográficos
Resumo: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.
Autores principais:Verissimo, Edite
Outros Autores:Berry, Neil; Gibbons, Peter D.; Cristiano, Maria Lurdes Santos; Rosenthal, Philip J.; Gut, Jiri; Ward, Stephen A.; O'Neill, Paul M.
Assunto:Malaria Plasmodium falciparum Cysteine protease Falcipain-2 Peptidomimetic
Ano:2008
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso restrito
Instituição associada:Universidade do Algarve
Idioma:inglês
Origem:Sapientia - Universidade do Algarve
Descrição
Resumo: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.