Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 148, Issue -, Pages 39-53Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.02.021
Keywords
Pyrimidine hybrids; 7-Chloroquinoline; Triazole; Huisgen 1,3-dipolar cycloaddition; Antiplasmodial studies; Lipophilicity; Binding with DNA
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Funding
- CSIR, New Delhi [01(2687) 12 EMR-II]
- University of Cape Town
- South African Medical Research Council
- South African Research Chairs Initiative of the Department of Science and Technology
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Triazole tethered 7-chloroquinoline-pyrimidine-5-carboxylate hybrids were synthesized and evaluated for antiplasmodial activity against chloroquine sensitive (CQ(s)) NF54 strain of Plasmodium falciparum. The most active hybrids of the series were further screened against the chloroquine resistant (CQ(R)) Dd2 strain of the parasite and for in vitro cytotoxicity against mammalian Vero cell lines. Further, their physicochemical properties, binding studies with hemin (monomeric & mu-oxo dimeric) and DNA [pUC-18, calf thymus (CT)] led us to plausible proposed binding mode of the most active member of the present series. (C) 2018 Elsevier Masson SAS. All rights reserved.
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