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A Pantetheinase-Resistant Pantothenamide with Potent, On Target, and Selective Antiplasmodial Activity

Macuamule, Cristiano; Tjhin, Erick; Jana, Collins E.; Barnard, Leanne; Koekemoer, Lizbe; de Villiers, Marianne; Saliba, Kevin; Strauss, Erick

Description

Pantothenamides inhibit blood-stage Plasmodium falciparum with potencies (50% inhibitory concentration [IC50], 20 nM) similar to that of chloroquine. They target processes dependent on pantothenate, a precursor of the essential metabolic cofactor coenzyme A. However, their antiplasmodial activity is reduced due to degradation by serum pantetheinase. Minor modification of the pantothenamide structure led to the identification of -methyl-N-phenethyl-pantothenamide, a pantothenamide...[Show more]

CollectionsANU Research Publications
Date published: 2015
Type: Journal article
URI: http://hdl.handle.net/1885/31116
Source: Antimicrobial Agents and Chemotherapy
DOI: 10.1128/AAC.04970-14

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