In vitro activity of wALADin benzimidazoles against different life cycle stages of Plasmodium parasites.
Antimicrob Agents Chemother
; 59(1): 654-8, 2015 Jan.
Article
en En
| MEDLINE
| ID: mdl-25313210
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.
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MEDLINE
Asunto principal:
Plasmodium falciparum
/
Bencimidazoles
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Porfobilinógeno Sintasa
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Antimaláricos
Límite:
Humans
Idioma:
En
Año:
2015
Tipo del documento:
Article