1H-1,2,3-三唑连接的异吲哚酮-7-氯喹啉和3-羟基吲哚-7-氯喹啉缀合物：合成与抗疟活性评价
1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: synthesis and antimalarial evaluation.
作者信息
Raj Raghu, Gut Jiri, Rosenthal Philip J, Kumar Vipan
机构信息
Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, Punjab, India.
Department of Medicine, University of California, San Francisco, CA, USA.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):756-9. doi: 10.1016/j.bmcl.2013.12.109. Epub 2014 Jan 3.
A series of 1H-1,2,3-triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates have been synthesized and evaluated for their antimalarial activity against chloroquine-resistant W2 strain of Plasmodium falciparum. The most potent of the test compound with an optimum combination of 3-hydroxy-indole ring and a n-butyl linker displayed an IC50 value of 69 nM.
一系列通过1H-1,2,3-三唑连接的异吲哚酮-7-氯喹啉和3-羟基吲哚-7-氯喹啉共轭物已被合成，并针对其对恶性疟原虫氯喹抗性W2株的抗疟活性进行了评估。测试化合物中最有效的一种，其3-羟基吲哚环和正丁基连接基的组合最佳，IC50值为69 nM。
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