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Shetty, R.V. et al.

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.[1]

References

Synthesis of 2-benzyloxy and 2-benzylthio analogues of primaquine as potential antimalarials. Shetty, R.V., Wetter, W.P., Blanton, C.D. J. Med. Chem. (1977) [Pubmed]

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