4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 3, Pages 756-759

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.109

Keywords

7-Chloroquinoline; Isatin; 3-Hydroxy-indole-2-one; 1H-1,2,3-Triazole; Antimalarial activity

Funding

  1. Board of Research in Nuclear Sciences under DAE Research Award

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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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