1056898-64-6Relevant academic research and scientific papers
Imidazolidin-4-one peptidomimetic derivatives of primaquine: Synthesis and antimalarial activity
Vale, Nuno,Matos, Joana,Gut, Jiri,Nogueira, Fatima,do Rosario, Virgilio,Rosenthal, Philip J.,Moreira, Rui,Gomes, Paula
body text, p. 4150 - 4153 (2009/04/10)
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 N1-acylation. Thus, 'internal' imidazolidin-4-ones derived from dipeptidyl 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships.
