AI Article Synopsis
- wALADin1 benzimidazoles are inhibitors of a key enzyme in Wolbachia bacteria found in filarial nematodes.
- These compounds demonstrated effectiveness against the blood stage of Plasmodium falciparum, with varying inhibitory concentrations.
- One derivative notably hindered the movement of sporozoites and their ability to invade liver cells, positioning wALADin1 as a valuable research tool and promising candidate for malaria treatment.
Article 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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|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4291411 | PMC |
| http://dx.doi.org/10.1128/AAC.02383-14 | DOI Listing |
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