2. Academic Validation
  3. Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents

  • Bioorg Med Chem Lett. 2017 Feb 1;27(3):658-661. doi: 10.1016/j.bmcl.2016.11.077.
Marlene Espinoza-Moraga 1,  Kawaljit Singh 1,  Mathew Njoroge 1,  Gurminder Kaur 1,  John Okombo 1,  Carmen De Kock 2,  Peter J Smith 2,  Sergio Wittlin 3,  Kelly Chibale 4
Affiliations

Affiliations

  • 1 Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
  • 2 Division of Clinical Pharmacology, Faculty of Health Sciences, University of Cape Town, K45, OMB, Groote Schuur Hospital, Observatory, 7925, South Africa.
  • 3 Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland; University of Basel, 4002 Basel, Switzerland.
  • 4 Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address: [email protected].
PMID: 28012840 DOI: 10.1016/j.bmcl.2016.11.077
Abstract

A series of novel fusidic acid (FA) derivatives was synthesized by replacing the carboxylic acid group with various ester and amide groups and evaluated in vitro for their antiplasmodial activity against the chloroquine-sensitive NF54 and multidrug-resistant K1 strains of the malarial parasite Plasmodium falciparum. Most of these derivatives showed a 4-49 and 5-17-fold increase in activity against NF54 and KI strains, respectively, as compared to FA and had a good selectivity index. These derivatives are stable over the incubation period and do not appear to be prodrugs of fusidic acid.

Keywords

Antiplasmodial; Fusidic acid; Malaria.

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