4.7 Article

1H-1,2,3-triazole tethered isatin-ferrocene conjugates: Synthesis and in vitro antimalarial evaluation

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 87, 期 -, 页码 801-804

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ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.10.024

关键词

Isatin-ferrocene conjugates; Click chemistry; Structure activity relationship; Antimalarial evaluation; Cytotoxicity

资金

  1. Department of Science and Technology, New Delhi [IF-10482]

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1H-1,2,3-triazole tethered isatin-ferrocene conjugates were synthesized and evaluated for their anti-plasmodial activities against chloroquine-susceptible (3D7) and chloroquine-resistant (W2) strains of Plasmodium falciparum. The conjugates 5f and 5h with an optimum combination of electron-withdrawing halogen substituent at C-5 position of isatin ring and a propyl chain, introduced as linker, proved to be most potent and non-cytotoxic among the series with IC50 values of 3.76 and 4.58 mu M against 3D7 and W2 strains, respectively. (c) 2014 Elsevier Masson SAS. All rights reserved.

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