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Issue 11, 2015
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Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G

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Abstract

A series of fusidic acid derivatives was synthesized by replacing the carboxylic acid group with various bioisosteres and evaluated in vitro against the chloroquine-sensitive NF54 strain of malaria parasite Plasmodium falciparum. Most of these derivatives showed a 2–35 fold increase in activity as compared to fusidic acid and had a good selectivity index. Further, docking experiments of fusidic acid and the most active derivative 18 within the active site of plasmodial elongation factor-Gs suggested that the binding orientation of 18 is similar to fusidic acid, but with slightly better docking score.

Graphical abstract: Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G

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Publication details

The article was received on 13 Aug 2015, accepted on 05 Oct 2015 and first published on 13 Oct 2015


Article type: Concise Article
DOI: 10.1039/C5MD00343A
Author version available: Download Author version (PDF)
Citation: Med. Chem. Commun., 2015,6, 2023-2028
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    Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G

    G. Kaur, K. Singh, E. Pavadai, M. Njoroge, M. Espinoza-Moraga, C. De Kock, P. J. Smith, S. Wittlin and K. Chibale, Med. Chem. Commun., 2015, 6, 2023
    DOI: 10.1039/C5MD00343A

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