The nematode serotonin-gated chloride channel MOD-1: A novel target for anthelmintic therapy

Araujo, Noelia Rodriguez; Hernando, Guillermina; Corradi, Jeremías; Bouzat, Cecilia

doi:10.1016/j.jbc.2022.102356

Cited by 2 publications

(1 citation statement)

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“…Locomotion assays : Motility assays were performed with wMicroTracker (Phylumtech S.A, Argentina), which is a LED‐based assay system that allows nematode motility to be recorded over time [76,77] . All assays were done at room temperature (21–23 °C) with young adult hermaphrodite worms from synchronized plates.…”

Section: Methodsmentioning

confidence: 99%

Potent Anthelmintic Activity of Chalcones Synthesized by an Effective Green Approach

Turani,

Castro,

Vazzana

et al. 2024

ChemMedChem

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There is currently an urgent need for new anthelmintic agents due to increasing resistance to the limited available drugs. The chalcone scaffold is a privileged structure for developing new drugs and has been shown to exhibit potential antiparasitic properties. We synthesized a series of chalcones via Claisen‐Schmidt condensation, introducing a novel recoverable catalyst derived from biochar obtained from the pyrolysis of tree pruning waste. Employing microwave irradiation and a green solvent, this approach demonstrated significantly reduced reaction times and excellent compatibility with various functional groups. The result was the generation of a library of functionalized chalcones, exhibiting exclusive (E)‐selectivity and high to excellent yields. The chalcone derivatives were evaluated on the free‐living nematode Caenorhabditis elegans. The chalcone scaffold, along with two derivatives incorporating a methoxy substituent in either ring, caused a concentration‐dependent decrease of worm motility, revealing potent anthelmintic activity and spastic paralysis not mediated by the nematode levamisole‐sensitive nicotinic receptor. The combination of both methoxy groups in the chalcone scaffold resulted in a less potent compound causing worm hypermotility at the short term, indicating a distinct molecular mechanism. Through the identification of promising drug candidates, this work addresses the demand for new anthelmintic drugs while promoting sustainable chemistry.

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Section: Methodsmentioning

confidence: 99%