In VitroActivity of wALADin Benzimidazoles against Different Life Cycle Stages of Plasmodium Parasites

Abstract

ABSTRACTwALADin1 benzimidazoles are specific inhibitors of δ-aminolevulinic acid dehydratase fromWolbachiaendobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stagePlasmodium falciparumin vitro(50% inhibitory concentrations, 39, 7.7, and 12.8 μM, respectively). One of these derivatives inhibited gliding motility ofPlasmodium bergheiANKA infectious sporozoites with nanomolar affinity and blocked invasion into hepatocytes but did not affect intrahepatocytic replication. Hence, wALADin1 benzimidazoles are tools to study gliding motility and potential antiplasmodial drug candidates.