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NOT Open Access | Toward a Stable and Potent Coenzyme A-Targeting Antiplasmodial Agent: Structure-Activity Relationship Studies of N-Phenethyl-α-methyl-pantothenamide

July 15, 2020 - 14:32 -- NOT Open Access
Spry C, Barnard L, Kok M, Powell AK, Mahesh D, Tjhin ET, Saliba KJ, Strauss E, de Villiers M
ACS Infect Dis. 2020 Jul 10;6(7):1844-1854

Pantothenamides (PanAms) are potent antiplasmodials with low human toxicity currently being investigated as antimalarials with a novel mode of action. These structural analogues of pantothenate, the vitamin precursor of the essential cofactor coenzyme A, are susceptible to degradation by pantetheinase enzymes present in serum. We previously discovered that α-methylation of the β-alanine moiety of PanAms increases their stability in serum and identified N-phenethyl-α-methyl-pantothenamide as a pantetheinase-resistant PanAm with potent, on-target, and selective antiplasmodial activity.

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