Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21198
Título: Artemisinin-dipeptidyl vinyl sulfone hybrid molecules
Design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition
Autor: Capela, Rita
Oliveira, Rudi
Goncalves, Lidia M.
Domingos, Ana
Gut, Jiri
Rosenthal, Philip J.
Lopes, Francisca
Moreira, Rui
Palavras-chave: Chemistry, Medicinal
Chemistry, Organic
Data: 2009
Editora: PERGAMON-ELSEVIER SCIENCE LTD
Citação: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 19, n. 12 (2009), p. 3229-3232
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.
URI: http://hdl.handle.net/10451/21198
DOI: http://dx.doi.org/10.1016/j.bmcl.2009.04.100
ISSN: 0960-894X
Aparece nas colecções:FF - Produção Científica 2000-2009

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