Orientador(es)
Resumo(s)
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.
Descrição
Palavras-chave
Chemistry, Medicinal Chemistry, Organic
Contexto Educativo
Citação
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 18, n. 14 (2008), p. 4150-4153
Editora
PERGAMON-ELSEVIER SCIENCE LTD