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2-取代伯氨喹类似物作为潜在抗疟药的合成。

Synthesis of 2-substituted primaquine analogues as potential antimalarials.

作者信息

Shetty R V, Blanton C D

出版信息

J Med Chem. 1978 Sep;21(9):995-8. doi: 10.1021/jm00207a030.

DOI:10.1021/jm00207a030
PMID:102798
Abstract

A series of 2-substituted primaquine analogues has been synthesized and evaluated against Plasmodium berghei in the mouse and Leishmania donovani in the hamster. Three members (3a,d,e) of the series were evaluated against Plasmodium cynomolgi in the rhesus monkey. One analogue (3d) was evaluated against Trypanosoma rhodesiense in the mouse, and two (3b,e) were evaluated against Schistosoma mansoni in the mouse. Several analogues possessed significant activity against P. berghei (3e,f) and L. donovani (3a,e).

摘要

已合成了一系列2-取代的伯氨喹类似物，并在小鼠体内针对伯氏疟原虫以及在仓鼠体内针对杜氏利什曼原虫进行了评估。该系列中的三个成员（3a、d、e）在恒河猴体内针对食蟹猴疟原虫进行了评估。一种类似物（3d）在小鼠体内针对罗德西亚锥虫进行了评估，两种（3b、e）在小鼠体内针对曼氏血吸虫进行了评估。几种类似物对伯氏疟原虫（3e、f）和杜氏利什曼原虫（3a、e）具有显著活性。

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