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Issue 3, 2019
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Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles

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Abstract

Analogues of a novel class of benzimidazoles with an intramolecular hydrogen bonding motif have been synthesized and evaluated in vitro for their antiplasmodium activity against chloroquine-sensitive (NF54) and multi-drug resistant (K1) strains of the human malaria parasite Plasmodium falciparum. Compounds were also screened for their cytotoxicity towards a mammalian Chinese hamster ovarian (CHO) cell line. Most of the compounds exhibited good antiplasmodium activity (PfNF54 IC50 <1 μM) and were relatively noncytotoxic. Moreover, towards establishing the possible mode of action of these molecules, inhibition of beta-hematin formation was investigated and two compounds were found to be inhibitors. Single crystal X-ray data confirmed the existence of an intramolecular hydrogen bond.

Graphical abstract: Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles

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Publication details

The article was received on 10 Dec 2018, accepted on 14 Feb 2019 and first published on 19 Feb 2019


Article type: Research Article
DOI: 10.1039/C8MD00608C
Med. Chem. Commun., 2019,10, 450-455

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    Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles

    H. D. Attram, S. Wittlin and K. Chibale, Med. Chem. Commun., 2019, 10, 450
    DOI: 10.1039/C8MD00608C

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