Artemisinin-dipeptidyl vinyl sulfone hybrid molecules

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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