The Invention of WM382, a Highly Potent PMIX/X Dual Inhibitor toward the Treatment of Malaria

Abstract excerpt

Drug resistance to first-line antimalarials─including artemisinin─is increasing, resulting in a critical need for the discovery of new agents with novel mechanisms of action. In collaboration with the Walter and Eliza Hall Institute and with funding from the Wellcome Trust, a phenotypic screen of Merck’s aspartyl protease inhibitor library identified a series of plasmepsin X (PMX) hits that were more potent than...

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