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Article

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

by 1,2, 3,4,5, 3,4,5 and 1,2,*
1
Institut für Medizinische und Pharmazeutische Chemie, Technische Universität Braunschweig, 38106 Braunschweig, Germany
2
Zentrum für Pharmaverfahrenstechnik (PVZ), Technische Universität Braunschweig, Franz-Liszt-Straße 35A, 38106 Braunschweig, Germany
3
Centre for Structural Systems Biology, 22607 Hamburg, Germany
4
Bernhard Nocht Institute for Tropical Medicine, 20359 Hamburg, Germany
5
Department of Biology, University of Hamburg, 20146 Hamburg, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Branka Zorc
Molecules 2020, 25(14), 3187; https://doi.org/10.3390/molecules25143187
Received: 16 June 2020 / Revised: 1 July 2020 / Accepted: 2 July 2020 / Published: 13 July 2020
(This article belongs to the Special Issue Purposing and Repurposing of Antimalarial Agents)
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). View Full-Text
Keywords: anti-malarial drugs; antiplasmodial; malaria; PfGSK-3; Plasmodium falciparum; thieno[2,3-b]pyridine; Thorpe-Ziegler reaction anti-malarial drugs; antiplasmodial; malaria; PfGSK-3; Plasmodium falciparum; thieno[2,3-b]pyridine; Thorpe-Ziegler reaction
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MDPI and ACS Style

Schweda, S.I.; Alder, A.; Gilberger, T.; Kunick, C. 4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents. Molecules 2020, 25, 3187. https://doi.org/10.3390/molecules25143187

AMA Style

Schweda SI, Alder A, Gilberger T, Kunick C. 4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents. Molecules. 2020; 25(14):3187. https://doi.org/10.3390/molecules25143187

Chicago/Turabian Style

Schweda, Sandra I., Arne Alder, Tim Gilberger, and Conrad Kunick. 2020. "4-Arylthieno[2,3-b]pyridine-2-carboxamides Are a New Class of Antiplasmodial Agents" Molecules 25, no. 14: 3187. https://doi.org/10.3390/molecules25143187

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