Issue 11, 2015

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

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

Supplementary files

Article information

Article type
Concise Article
Submitted
13 Aug 2015
Accepted
05 Oct 2015
First published
13 Oct 2015

Med. Chem. Commun., 2015,6, 2023-2028

Author version available

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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