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

被引：66
作者：
Raj, Raghu [1 ]
Gut, Jiri [2 ]
Rosenthal, Philip J. [2 ]
Kumar, Vipan [1 ]
机构：
[1] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India
[2] Univ Calif San Francisco, Dept Med, San Francisco, CA USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 03期
关键词：
7-Chloroquinoline; Isatin; 3-Hydroxy-indole-2-one; 1H-1,2,3-Triazole; Antimalarial activity; IN-VITRO; HYBRID MOLECULES; INHIBITORS; POTENT; DESIGN; ISATIN; SPIROINDOLONES; IDENTIFICATION; OXINDOLES; MALARIA;
D O I：
10.1016/j.bmcl.2013.12.109
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (C) 2013 Elsevier Ltd. All rights reserved.
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页码：756 / 759
页数：4
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