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Ookluc: A Plasmodium berghei Line for Identifying Transmission-blocking Compounds
Published on: July 11, 2025
2,4-Diaminothienopyrimidines as orally active antimalarial agents
Diego González Cabrera1, Claire Le Manach, Frederic Douelle
1Department of Chemistry and ■Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.
Abstract:
A novel series of 2,4-diaminothienopyrimidines with potential as antimalarials was identified from whole-cell high-throughput screening of a SoftFocus ion channel library. Synthesis and structure-activity relationship studies identified compounds with potent antiplasmodial activity and low in vitro cytotoxicity. Several of these analogues exhibited in vivo activity in the Plasmodium berghei mouse model when administered orally. However, inhibition of the hERG potassium channel was identified as a liability for this series.
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