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

被引：68

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.

引用

页码：756 / 759

页数：4

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