1977•Journal of Medicinal ChemistryRequires access
Synthesis of 2-benzyloxy and 2-benzylthio analogs of primaquine as potential antimalarials
Raghav V. Shetty, William P. Wetter, C. DeWitt Blanton
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Abstract
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.