Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones.
A series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 microg/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the muM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead compound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.
Vale
Nuno
N
CIQUP-Centro de Investigação em Química da Universidade do Porto, Departamento de Química, Faculdade de Ciências, Universidade do Porto, P-4169-007 Porto, Portugal.
Collins
Margaret S
MS
Gut
Jiri
J
Ferraz
Ricardo
R
Rosenthal
Philip J
PJ
Cushion
Melanie T
MT
Moreira
Rui
R
Gomes
Paula
P
D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology*; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D048288:Imidazolines / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D045363:Pneumocystis carinii / Q000187:drug effects*; D011319:Primaquine / Q000737:chemistry / Q000494:pharmacology*
D000935:Antifungal Agents; D000962:Antimalarials; D048288:Imidazolines; D011319:Primaquine