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Artemisinin-dipeptidyl vinyl sulfone hybrid molecules

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Resumo:A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened for antiplasmodial activity and falcipain-2 inhibition. All conjugates were active against the Plasmodium falciparum W2 strain in the low nanomolar range and those containing the Leu-hPhe core inhibited falcipain-2 in low micromolar range. (C) 2009 Elsevier Ltd. All rights reserved.. - FCT (Portugal) [SFRH/BD/30418/2006]; National Institutes of Health. - This work was supported by FCT (Portugal) and the National Institutes of Health; R. C. acknowledges FCT for the PhD grant SFRH/BD/30418/2006. PJR is a Doris Duke Charitable Foundation Distinguished Clinical Scientist.
Autores principais:Capela, Rita
Outros Autores:Oliveira, Rudi; Goncalves, Lidia M.; Domingos, Ana; Gut, Jiri; Rosenthal, Philip J.; Lopes, Francisca; Moreira, Rui
Assunto:Chemistry, Medicinal Chemistry, Organic
Ano:2009
País:Portugal
Tipo de documento:artigo
Tipo de acesso:acesso a metadados
Instituição associada:Universidade de Lisboa
Idioma:inglês
Origem:Repositório da Universidade de Lisboa

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