Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials.
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.
Araújo
Maria João
MJ
CIQUP, Department of Chemistry, Faculty of Sciences, University of Oporto, Rua do Campo Alegre 687, 4169-007 Porto, Portugal.
Bom
Joana
J
Capela
Rita
R
Casimiro
Catarina
C
Chambel
Paula
P
Gomes
Paula
P
Iley
Jim
J
Lopes
Francisca
F
Morais
José
J
Moreira
Rui
R
de Oliveira
Eliandre
E
do Rosário
Virgílio
V
Vale
Nuno
N
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
D000962:Antimalarials; D048289:Imidazolidines; D011319:Primaquine