抗疟药。11. 作为潜在抗疟药的3-氨基喹啉和5-氨基喹啉的合成。

Antimalarials. 11. Synthesis of 3- and 5-aminoquinolines as potential antimalarials.

作者信息

Khan M S, LaMontagne M P

出版信息

J Med Chem. 1979 Aug;22(8):1005-8. doi: 10.1021/jm00194a024.

Abstract

A series of 3-quinolinediamines (1g, 2c, and 3e) structurally related to primaquine and 4-methylprimaquine have been prepared and tested for antimalarial activity against Plasmodium berghei in mice and antileishmanial activity against Leishmania donovani in the hamster. All were inactive. In addition, three 5-quinolinediamines (4b, 5, and 6) were prepared. All were inactive against Leishmania donovani in hamsters. One of the examples, 6, was curative against Plasmodium cynmolgi in the rhesus monkey.

摘要

已制备了一系列在结构上与伯氨喹和4-甲基伯氨喹相关的3-喹啉二胺（1g、2c和3e），并测试了它们对小鼠伯氏疟原虫的抗疟活性以及对仓鼠杜氏利什曼原虫的抗利什曼活性。所有化合物均无活性。此外，还制备了三种5-喹啉二胺（4b、5和6）。所有这些化合物对仓鼠杜氏利什曼原虫均无活性。其中一个例子，即化合物6，对恒河猴食蟹疟原虫具有治愈作用。