title: Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials.
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.
authors.affiliation: CIQUP, Department of Chemistry, Faculty of Sciences, University of Oporto, Rua do Campo Alegre 687, 4169-007 Porto, Portugal.
authors.forename: Maria João
authors.initials: MJ
authors.lastname: Araújo
authors.forename: Joana
authors.initials: J
authors.lastname: Bom
authors.forename: Rita
authors.initials: R
authors.lastname: Capela
authors.forename: Catarina
authors.initials: C
authors.lastname: Casimiro
authors.forename: Paula
authors.initials: P
authors.lastname: Chambel
authors.forename: Paula
authors.initials: P
authors.lastname: Gomes
authors.forename: Jim
authors.initials: J
authors.lastname: Iley
authors.forename: Francisca
authors.initials: F
authors.lastname: Lopes
authors.forename: José
authors.initials: J
authors.lastname: Morais
authors.forename: Rui
authors.initials: R
authors.lastname: Moreira
authors.forename: Eliandre
authors.initials: E
authors.lastname: de Oliveira
authors.forename: Virgílio
authors.initials: V
authors.lastname: do Rosário
authors.forename: Nuno
authors.initials: N
authors.lastname: Vale
mesh_terms: D000818:Animals; D000852:Anopheles / Q000469:parasitology; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004355:Drug Stability; D006801:Humans; D048289:Imidazolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D066298:In Vitro Techniques; D008288:Malaria / Q000097:blood / Q000188:drug therapy; D051379:Mice; D008807:Mice, Inbred BALB C; D010962:Plasmodium berghei / Q000187:drug effects; D011319:Primaquine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000962:Antimalarials; D048289:Imidazolidines; D011319:Primaquine