4,5-二取代伯氨喹类似物作为潜在的抗原生动物药物。

4,5-disubstituted primaquine analogs as potential antiprotozoan agents.

作者信息

Burghard H, DeWitt Blanton C

出版信息

J Pharm Sci. 1980 Aug;69(8):933-6. doi: 10.1002/jps.2600690818.

Abstract

4,5-Dimethylprimaquine and 5-fluoro-4-methylprimaquine were synthesized and evaluated against Plasmodium berghei in the mouse. Significant blood schizonticidal activity was observed. The 5-fluoro-4-methylprimaquine analog also was active as a tissue schizonticidal agent when evaluated against P. cynomolgi in the rhesus monkey, as an antileishmanial agent when evaluated against Leishmania donovani in the hamster, and as a causal prophylactic agent when evaluated against P. berghei yoelii.

摘要

合成了4,5-二甲基伯氨喹和5-氟-4-甲基伯氨喹，并在小鼠体内对伯氏疟原虫进行了评估。观察到显著的血内裂殖体杀灭活性。当在恒河猴体内对食蟹猴疟原虫进行评估时，5-氟-4-甲基伯氨喹类似物作为组织裂殖体杀灭剂具有活性；当在仓鼠体内对杜氏利什曼原虫进行评估时，它作为抗利什曼原虫剂具有活性；当对约氏疟原虫进行评估时，它作为病因性预防剂具有活性。