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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Espinoza-Moraga M,Singh K,Njoroge M,Kaur G,Okombo J,De Kock C,Smith PJ,Wittlin S,Chibale K

doi

10.1016/j.bmcl.2016.11.077

subject

Has Abstract

pub_date

2017-02-01 00:00:00

pages

658-661

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)31241-0

journal_volume

27

pub_type

杂志文章

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