Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones

Vale, Nuno; Collins, Margaret S.; Gut, Jiri; Ferraz, Ricardo; Rosenthal, Philip J.; Cushion, Melanie T.; Moreira, Rui; Gomes, Paula

http://hdl.handle.net/10400.22/20459

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Abstract(s)

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 lg/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 lM range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead com pound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation.

Keywords

AIDS Antimalarial Antiplasmodial HIV Infection Malaria Plasmodium falciparum Pneumocystis carinii Primaq

URI

http://hdl.handle.net/10400.22/20459

Citation

Vale, N., Collins, M. S., Gut, J., Ferraz, R., Rosenthal, P. J., Cushion, M. T., Moreira, R., & Gomes, P. (2008). Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones. Bioorganic & Medicinal Chemistry Letters, 18(2), 485-488. https://doi.org/https://doi.org/10.1016/j.bmcl.2007.11.105