一系列新型三氧喹啉的合成及其抗疟活性
Synthesis and antimalarial activity of a new series of trioxaquines.
作者信息
Singh Chandan, Malik Heetika, Puri Sunil K
机构信息
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow-226001, India.
出版信息
Bioorg Med Chem. 2004 Mar 1;12(5):1177-82. doi: 10.1016/j.bmc.2003.11.021.
PMID:14980628
Abstract
Trioxanes 8a-b, easily accessible in two steps from allylic alcohol 6a-b, on reductive amination with 4-aminoquinolines 4a-c furnish a new series of trioxaquines 9a-b, 10a-b, 11a-b in 32-77% yields. Dicitrate salts of these trioxaquines have been evaluated for antimalarial activity against multidrug resistant Plasmodium yoelii in mice model.
摘要
从烯丙醇6a - b经两步反应即可轻松制得的三聚甲醛8a - b，与4 - 氨基喹啉4a - c进行还原胺化反应，以32 - 77%的产率得到了一系列新的三氧喹啉9a - b、10a - b、11a - b。已在小鼠模型中对这些三氧喹啉的二柠檬酸盐进行了针对多重耐药约氏疟原虫的抗疟活性评估。
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