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Related Experiment Videos

Anticoccidial activity of crown polyethers.

G R Brown, A J Foubister

    Journal of Medicinal Chemistry
    |April 1, 1983
    PubMed
    Summary

    Crown polyethers show promising in vitro anticoccidial activity against Eimeria tenella. However, these compounds were not effective in vivo, suggesting further research is needed for practical applications.

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    Area of Science:

    • Veterinary Parasitology
    • Medicinal Chemistry

    Background:

    • Coccidiosis, caused by Eimeria parasites, poses a significant threat to poultry health and welfare.
    • Developing novel anticoccidial agents is crucial to combat resistance and improve treatment efficacy.

    Purpose of the Study:

    • To evaluate the in vitro anticoccidial activity of crown polyethers against Eimeria tenella.
    • To investigate the structure-activity relationship of crown polyethers based on their ring sizes.

    Main Methods:

    • In vitro screening of crown polyethers with varying ring sizes (14-30 atoms) against Eimeria tenella.
    • Determination of minimum inhibitory concentrations (MICs) for active compounds.
    • In vivo testing of selected potent compounds in a relevant animal model.

    Main Results:

    • Crown polyethers demonstrated significant in vitro anticoccidial activity, with compounds 4 and 9 being the most potent, active at 0.33 ppm.
    • No anticoccidial activity was observed in vivo for any of the tested crown polyethers.
    • The efficacy appears related to the lipophilic shielding of complexed cations, influencing in vitro activity.

    Conclusions:

    • Crown polyethers exhibit potent in vitro anticoccidial properties against Eimeria tenella.
    • The lack of in vivo efficacy suggests limitations in bioavailability or target engagement in a living organism.
    • Further studies are warranted to explore modifications or delivery systems to enhance in vivo performance.

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