Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21199
Título: Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials
Autor: Rodrigues, Tiago
Guedes, Rita C.
dos Santos, Daniel J. V. A.
Carrasco, Marta
Gut, Jiri
Rosenthal, Philip J.
Moreira, Rui
Lopes, Francisca
Palavras-chave: Chemistry, Medicinal
Chemistry, Organic
Data: 2009
Editora: PERGAMON-ELSEVIER SCIENCE LTD
Citação: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 19, n. 13 (2009), p. 3476-3480
Resumo: (1H-Pyridin-4-ylidene)amines containing lipophilic side chains at the imine nitrogen atom were prepared as potential clopidol isosteres in the development of antimalarials. Their antiplasmodial activity was evaluated in vitro against the Plasmodium falciparum W2 (chloroquine-resistant) and FCR3 (atovaquone-resistant) strains. The most active of these derivatives, 4m, had an IC50 of 1 mu M against W2 and 3 mu M against FCR3. Molecular modeling studies suggest that (1H-pyridin-4-ylidene) amines may bind to the ubiquinol oxidation Q(o) site of cytochrome bc(1). (C) 2009 Elsevier Ltd. All rights reserved.. - Funda ao para a Ciencia e Tecnologia (FCT, Portugal) ; Doris Duke Charitable Foundation Distinguished Clinical Scientist [SFRH/BD/30689/2006]. - This work was supported by Funda ao para a Ciencia e Tecnologia (FCT, Portugal); T. R. acknowledges FCT for the Ph. D. grant SFRH/BD/30689/2006. P.J.R. is a Doris Duke Charitable Foundation Distinguished Clinical Scientist.
URI: http://hdl.handle.net/10451/21199
DOI: http://dx.doi.org/10.1016/j.bmcl.2009.05.017
ISSN: 0960-894X
Aparece nas colecções:FF - Produção Científica 2000-2009

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