Triazole Substitution of a Labile Amide Bond Stabilizes Pantothenamides and Improves Their Antiplasmodial Potency.

@article{Howieson2016TriazoleSO,
  title={Triazole Substitution of a Labile Amide Bond Stabilizes Pantothenamides and Improves Their Antiplasmodial Potency.},
  author={Vanessa M Howieson and Elisa Tran and Annabelle Hoegl and Han Ling Fam and Jonathan Fu and Kate Sivonen and Xiao Xuan Li and Karine Auclair and Kevin J. Saliba},
  journal={Antimicrobial agents and chemotherapy},
  year={2016},
  volume={60 12},
  pages={7146-7152}
}
The biosynthesis of coenzyme A (CoA) from pantothenate and the utilization of CoA in essential biochemical pathways represent promising antimalarial drug targets. Pantothenamides, amide derivatives of pantothenate, have potential as antimalarials, but a serum enzyme called pantetheinase degrades pantothenamides, rendering them inactive in vivo In this study… CONTINUE READING