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

Espinoza-Moraga, Marlene and Singh, Kawaljit and Njoroge, Mathew and Kaur, Gurminder and Okombo, John and De Kock, Carmen and Smith, Peter J. and Wittlin, Sergio and Chibale, Kelly. (2017) Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents. Bioorganic & medicinal chemistry, 27 (3). pp. 658-661.

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Official URL: http://edoc.unibas.ch/54442/

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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.
Faculties and Departments:09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH)
09 Associated Institutions > Swiss Tropical and Public Health Institute (Swiss TPH) > Department of Medical Parasitology and Infection Biology > Parasite Chemotherapy (Mäser)
UniBasel Contributors:Wittlin, Sergio
Item Type:Article, refereed
Publisher:Pergamon
ISSN:0968-0896
Note:Publication type according to Uni Basel Research Database: Journal article
Identification Number:
Last Modified:24 Apr 2017 14:24
Deposited On:24 Apr 2017 14:24

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