[抗疟 10 H-吲哚并(3,2 - b)喹啉 - 11 - 基 - 胺。1. 阿莫地喹和环氯喹类型的酚 - 曼尼希碱]
[Antimalarial 10 H-indolo(3,2-b)quinolin-11-yl-amines. 1. Phenol-Mannich-bases of the amodiaquine and cycloquine type].
作者信息
Görlitzer K, Stockmann R, Walter R D
机构信息
Institut für Pharmazeutische Chemie, Technischen Universität Braunschweig.
出版信息
Pharmazie. 1994 Apr;49(4):231-5.
The 11-chloro-quinoline derivatives 3 react with 4-aminophenol and the mono- and bis-phenol-Mannich-bases 6 to yield the 10H-indolo[3,2-b]quinoline-11-yl-amines 4 and 7. The amodiaquine analogue 7a as the best of all compounds shows a comparable activity with choroquine and inhibits a multiresistant Plasmodium falciparum strain at the same concentration. Compound 7e from the cycloquine-type was selected for an in vivo antitumor screening programme.
11 - 氯喹啉衍生物3与4 - 氨基酚以及单酚和双酚 - 曼尼希碱6反应，生成10H - 吲哚并[3,2 - b]喹啉 - 11 - 基胺4和7。作为所有化合物中最优者的阿莫地喹类似物7a表现出与氯喹相当的活性，并在相同浓度下抑制多重耐药恶性疟原虫菌株。来自环氯喹类型的化合物7e被选用于一项体内抗肿瘤筛选计划。
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