抗疟药。4. 三氯萘氨基醇。

Antimalarials. 4. Trichloronaphthalene amino alcohols.

作者信息

Shamblee D A, Gillespie J S

出版信息

J Med Chem. 1979 Jan;22(1):86-9. doi: 10.1021/jm00187a019.

Abstract

An improved procedure for the synthesis of naphthalene amino alcohols is described. Four new compounds were prepared and tested by Rane Laboratories for activity vs. Plasmodium berghei in mice. All compounds were active, the most active being 1-[3-(4-chlorophenyl)-5,7-dichloro-1-naphthyl]-3-(di-n-butylamino)propanol hydrochloride (16b). Structure--activity relationships between the naphthalene and quinoline isosteres are discussed.

摘要

描述了一种改进的萘氨基醇合成方法。制备了四种新化合物，并由瑞纳实验室测试了其对小鼠体内伯氏疟原虫的活性。所有化合物均有活性，其中活性最强的是1-[3-(4-氯苯基)-5,7-二氯-1-萘基]-3-(二正丁基氨基)丙醇盐酸盐(16b)。讨论了萘和喹啉等电子体之间的构效关系。