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

Araújo, Maria Joao; Bom, Joana; Capela, Rita; Casimiro, Catarina; Chambel, Paula; Gomes, Paula; Iley, Jim; Lopes, Francisca; Morais, Jose; Moreira, Rui; de Oliveira, Eliandre; do Rosário, Virgilio and Vale, Nuno (2005). Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials. Journal of Medicinal Chemistry, 48 pp. 888–892.

DOI (Digital Object Identifier) Link: http://dx.doi.org/10.1021/jm0494624
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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.

Item Type: Journal Article
ISSN: 0022-2623
Keywords: Imidazolidinones; Malaria
Academic Unit/Department: Science > Life, Health and Chemical Sciences
Item ID: 3986
Depositing User: James Iley
Date Deposited: 04 Jul 2006
Last Modified: 02 Dec 2010 19:50
URI: http://oro.open.ac.uk/id/eprint/3986
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