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2,4-diaminothienopyrimidines as orally active antimalarial agents
Journal
Journal of medicinal chemistry
Volume
57
Number
3
Pages / Article-Number
1014-1022
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.
