Synthesis of 2-benzyloxy and 2-benzylthio analogues of primaquine as potential antimalarials.
A series of 2-benzyloxy and 2-benzylthio analogues of primaquine has been synthesized and evaluated against Plasmodium berghei in the mouse and Plasmodium cynomolgi in the rhesus monkey. 8-Aminoquinoline toxicity, as measured in the Rane mouse screen, was reduced, and these compounds showed significant blood schizonticidal antimalarial activity in mice. In monkeys, significant tissue-schizonticidal activity was observed.
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis*; D000882:Haplorhini; D008288:Malaria / Q000188:drug therapy; D051379:Mice; D011319:Primaquine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D000962:Antimalarials; D011319:Primaquine