Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21672
Título: Imidazolidin-4-one peptidomimetic derivatives of primaquine
Synthesis and antimalarial activity
Autor: Vale, Nuno
Matos, Joana
Gut, Jiri
Nogueira, Fatima
do Rosario, Virgilio
Rosenthal, Philip J.
Moreira, Rui
Gomes, Paula
Palavras-chave: Chemistry, Medicinal
Chemistry, Organic
Data: 2008
Citação: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 18, n. 14 (2008), p. 4150-4153
Resumo: The synthesis of imidazolidin-4-one derivatives of primaquine containing the five-membered ring at the C-terminus of a dipeptide backbone coupled to the parent drug is described. These peptidomimetic derivatives were active against a chloroquine-resistant Plasmodium falciparum strain and inhibited the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The novel imidazolidin-4-ones are extremely stable, both in human plasma and in pH 7.4 buffer, as a result of N-1-acylation. Thus, 'internal' imidazolidin-4-ones derived from dipeptidyl 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships. (c) 2008 Elsevier Ltd. All rights reserved.
URI: http://hdl.handle.net/10451/21672
DOI: http://dx.doi.org/10.1016/j.bmcl.2008.05.076
ISSN: 0960-894X
Aparece nas colecções:FF - Produção Científica 2000-2009

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