1H-1,2,3-Triazole-tethered isatin-7-chloroquinoline and 3-hydroxy-indole-7-chloroquinoline conjugates: Synthesis and antimalarial evaluation

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• 作者：Raghu Raj ; Jiri Gut ; Philip J. Rosenthal ; Vipan Kumar
• 关键词：7-Chloroquinoline ; Isatin ; 3-Hydroxy-indole-2-one ; 1H-1 ; 2 ; 3-Triazole ; Antimalarial activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 February, 2014
• 年：2014
• 卷：24
• 期：3
• 页码：756-759
• 全文大小：531 K

文摘

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.