4,5-disubstituted primaquine analogs as potential antiprotozoan agents.
4,5-Dimethylprimaquine and 5-fluoro-4-methylprimaquine were synthesized and evaluated against Plasmodium berghei in the mouse. Significant blood schizonticidal activity was observed. The 5-fluoro-4-methylprimaquine analog also was active as a tissue schizonticidal agent when evaluated against P. cynomolgi in the rhesus monkey, as an antileishmanial agent when evaluated against Leishmania donovani in the hamster, and as a causal prophylactic agent when evaluated against P. berghei yoelii.
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D006224:Cricetinae; D000882:Haplorhini; D007898:Leishmaniasis, Visceral / Q000188:drug therapy; D008253:Macaca mulatta; D008288:Malaria / Q000188:drug therapy; D008647:Mesocricetus; D051379:Mice; D010961:Plasmodium / Q000187:drug effects; D010962:Plasmodium berghei; D011319:Primaquine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000981:Antiprotozoal Agents; D011319:Primaquine