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Tricyclic aryl-substituted anticoccidial azauracils.

A F Kluge, J M Caroon, S H Unger

    Journal of Medicinal Chemistry
    |June 1, 1978
    PubMed
    Summary

    New tricyclic 6-azauracils demonstrate anticoccidial effects against Eimeria species. Compound activity correlates with chemical shifts, not lipophilicity, offering potential for novel coccidiosis treatments.

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    Area of Science:

    • Medicinal Chemistry
    • Parasitology
    • Veterinary Pharmacology

    Background:

    • Coccidiosis, caused by Eimeria parasites, poses a significant threat to poultry health and productivity.
    • Development of novel anticoccidial agents is crucial for managing drug resistance and improving treatment efficacy.
    • Tricyclic aryl-substituted 6-azauracils represent a class of compounds with potential therapeutic applications.

    Purpose of the Study:

    • To synthesize and evaluate the anticoccidial activity of novel tricyclic aryl-substituted 6-azauracils.
    • To investigate the structure-activity relationship (SAR) of these compounds against Eimeria species.
    • To assess the in vivo and in vitro efficacy of a lead compound against Eimeria tenella and Eimeria brunetti.

    Main Methods:

    • Synthesis of a series of tricyclic aryl-substituted 6-azauracils.
    • Anticoccidial activity testing against Eimeria tenella and Eimeria necatrix.
    • Correlation analysis of compound activity with NMR chemical shifts and lipophilicity (logP).
    • In vivo and in vitro efficacy studies of the most active compound (Compound 23) against E. tenella and E. brunetti.

    Main Results:

    • Several synthesized compounds exhibited significant anticoccidial activity.
    • Anticoccidial activity correlated positively with the chemical shift of the azauracil ring proton, suggesting a specific mechanism of action.
    • No correlation was found between anticoccidial activity and compound lipophilicity.
    • Compound 23 demonstrated significant control of mortality (62 ppm) and weight gain reduction (31 ppm) in E. tenella infected chickens.
    • Compound 23 showed limited efficacy against E. brunetti and exerted a coccidiostatic effect in vitro.

    Conclusions:

    • Tricyclic aryl-substituted 6-azauracils are promising candidates for anticoccidial drug development.
    • The chemical shift of the azauracil ring proton serves as a valuable predictive marker for anticoccidial activity.
    • Compound 23 warrants further investigation as a potential therapeutic agent against Eimeria tenella infections.

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