Synthesis of 2-benzyloxy and 2-benzylthio analogues of primaquine as potential antimalarials.
作者信息
Shetty R V, Wetter W P, Blanton C D
出版信息
J Med Chem. 1977 Oct;20(10):1349-51. doi: 10.1021/jm00220a025.
PMID:409843
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.
摘要
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