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In vitro activity of wALADin benzimidazoles against different life cycle stages of Plasmodium parasites.

ABSTRACT: wALADin1 benzimidazoles are specific inhibitors of ?-aminolevulinic acid dehydratase from Wolbachia endobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stage Plasmodium falciparum in vitro (50% inhibitory concentrations, 39, 7.7, and 12.8 ?M, respectively). One of these derivatives inhibited gliding motility of Plasmodium berghei ANKA 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.

SUBMITTER: Lentz CS 

PROVIDER: S-EPMC4291411 | biostudies-literature | 2015 Jan

REPOSITORIES: biostudies-literature

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In vitro activity of wALADin benzimidazoles against different life cycle stages of Plasmodium parasites.

Lentz Christian S CS   Sattler Julia M JM   Fendler Martina M   Gottwalt Simon S   Halls Victoria S VS   Strassel Silke S   Arriens Sandra S   Hannam Jeffrey S JS   Specht Sabine S   Famulok Michael M   Mueller Ann-Kristin AK   Hoerauf Achim A   Pfarr Kenneth M KM  

Antimicrobial agents and chemotherapy 20141013 1

wALADin1 benzimidazoles are specific inhibitors of δ-aminolevulinic acid dehydratase from Wolbachia endobacteria of filarial nematodes. We report that wALADin1 and two derivatives killed blood stage Plasmodium falciparum in vitro (50% inhibitory concentrations, 39, 7.7, and 12.8 μM, respectively). One of these derivatives inhibited gliding motility of Plasmodium berghei ANKA infectious sporozoites with nanomolar affinity and blocked invasion into hepatocytes but did not affect intrahepatocytic r  ...[more]

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