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Structure-Activity Relationships of Antiplasmodial Pantothenamide Analogues Reveal a New Way by Which Triazoles Mimic Amide Bonds

Guan, Jinming; Tjhin, Erick; Howieson, Vanessa; Kittikool, Tanakorn; Spry, Christina; Saliba, Kevin; Auclair, Karine


Pantothenamides are potent growth inhibitors of the malaria parasite Plasmodium falciparum. Their clinical use is, however, hindered due to the ubiquitous presence of pantetheinases in human serum, which rapidly degrade pantothenamides into pantothenate and the corresponding amine. We previously reported that replacement of the labile amide bond with a triazole ring not only imparts stability toward pantetheinases, but also improves activity against P. falciparum. A small library of new...[Show more]

CollectionsANU Research Publications
Date published: 2018
Type: Journal article
Source: ChemMedChem
DOI: 10.1002/cmdc.201800327


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