4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents.

Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Sandra I SchwedaConrad Kunick

Abstract

Malaria causes hundreds of thousands of deaths every year, making it one of the most dangerous infectious diseases worldwide. Because the pathogens have developed resistance against most of the established anti-malarial drugs, new antiplasmodial agents are urgently needed. In analogy to similar antiplasmodial ketones, 4-arylthieno[2,3-b]pyridine-2-carboxamides were synthesized by Thorpe-Ziegler reactions. In contrast to the related ketones, these carboxamides are only weak inhibitors of the plasmodial enzyme PfGSK-3 but the compounds nevertheless show strong antiparasitic activity. The most potent representatives inhibit the pathogens with IC50 values in the two-digit nanomolar range and exhibit high selectivity indices (>100).

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Citations

Nov 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Giovanni BenelliAngelo Canale
Jun 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Serena MontanariAngela Rampa
Jun 15, 2021·ACS Omega·Tatyana A StroganovaGennady D Krapivin
Aug 28, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Duc Hoàng LandeConrad Kunick

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Methods Mentioned

BETA
column chromatography
differential scanning calorimetry
column chromatographies
Assay
flow cytometry

Software Mentioned

GraphPad Prism
GraphPad

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