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American Chemical Society, Journal of Medicinal Chemistry, 3(48), p. 888-892, 2005

DOI: 10.1021/jm0494624

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Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials

Journal article published in 2005 by Mj Araujo, Joana Bom, Rita Capela, Catarina Casimiro, Paula Chambel, Paula Gomes, Jim Iley, Francisca Lopes, José Morais, Rui Moreira ORCID, Eliandre de Oliveira ORCID, Virgílio do Rosário, Virgílio Do Rosario, Nuno Vale
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Imidazolidin-4-one derivatives of primaquine were synthesized as potential double prodrugs of the parent drug. The title compounds inhibit the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The imidazolidin-4-ones are very stable, both in human plasma and in pH 7.4 buffer, indicating that they are active per se. Thus, imidazolidin-4-ones derived from 8-aminoquinolines represent a new entry in antimalarial structure-activity relationships.