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antiplasmodial pantothenamides

NOT Open Access | Exploring Heteroaromatic Rings as a Replacement for the Labile Amide of Antiplasmodial Pantothenamides

April 6, 2021 - 14:29 -- NOT Open Access
Author(s): 
Guan J, Spry C, Auclair K, et al.
Reference: 
J Med Chem. 2021 Apr 1

Malaria-causing Plasmodium parasites are developing resistance to antimalarial drugs, providing the impetus for new antiplasmodials. Although pantothenamides show potent antiplasmodial activity, hydrolysis by pantetheinases/vanins present in blood rapidly inactivates them. We herein report the facile synthesis and biological activity of a small library of pantothenamide analogues in which the labile amide group is replaced with a heteroaromatic ring.

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