合成伯氨喹的2-苄氧基和2-苄硫基类似物作为潜在抗疟药。

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.

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

已合成了一系列伯氨喹的2-苄氧基和2-苄硫基类似物，并在小鼠体内针对伯氏疟原虫以及在恒河猴体内针对食蟹猴疟原虫进行了评估。如在Rane小鼠筛选试验中所测定的，8-氨基喹啉毒性降低，并且这些化合物在小鼠体内显示出显著的血液裂殖体杀灭抗疟活性。在猴子体内，观察到了显著的组织裂殖体杀灭活性。