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Avermectin acyl derivatives with anthelmintic activity

H Mrozik, P Eskola, M H Fisher

    Journal of Medicinal Chemistry
    |June 1, 1982
    PubMed
    Summary
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    Acetylation of avermectins A2a, B1a, and B2a yielded various derivatives. Certain 4"-acetylated avermectins demonstrated significant anthelmintic activity, particularly against Trichostrongylus colubriformis.

    Area of Science:

    • Organic Chemistry
    • Medicinal Chemistry
    • Parasitology

    Background:

    • Avermectins are potent anthelmintic compounds.
    • Chemical modification of avermectins can alter their activity and properties.

    Purpose of the Study:

    • To synthesize and characterize novel avermectin derivatives.
    • To evaluate the anthelmintic activity of these derivatives against parasitic nematodes.

    Main Methods:

    • Acetylation of avermectins A2a, B1a, and B2a.
    • Structure elucidation using 300-MHz 1H NMR and mass spectrometry.
    • Anthelmintic activity testing in gerbils and sheep models.

    Main Results:

    • Synthesis of various mono-, di-, and tri-acetylated avermectin derivatives.

    Related Experiment Videos

  • Identification of 4"-acetylated derivatives (4 and 7) with good anthelmintic activity.
  • Preparation of additional 4"-acylated derivatives of avermectin B1a, with some showing comparable potency to the parent compound against Trichostrongylus colubriformis.

    • Conclusions:

    • Chemical modification, specifically 4"-acetylation, can enhance or maintain anthelmintic potency.
    • Substitution or loss of the 5-hydroxy group significantly reduces activity.
    • Novel avermectin derivatives show promise for controlling parasitic infections.