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

Abstract:

: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 replication. Hence, wALADin1 benzimidazoles are tools to study gliding motility and potential antiplasmodial drug candidates.

authors

Lentz CS,Sattler JM,Fendler M,Gottwalt S,Halls VS,Strassel S,Arriens S,Hannam JS,Specht S,Famulok M,Mueller AK,Hoerauf A,Pfarr KM

doi

10.1128/AAC.02383-14

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

654-8

issue

1

eissn

0066-4804

issn

1098-6596

pii

AAC.02383-14

journal_volume

59

pub_type

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