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Hypolipidemic arylthioalkanoic acids

E R Wagner, R G Dull, L G Mueller

    Journal of Medicinal Chemistry
    |August 1, 1977
    PubMed
    Summary
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    Researchers investigated arylthioalkanoic acids for hypolipidemic activity. Compound 7, a specific hexanoic acid derivative, demonstrated optimal serum cholesterol and triglyceride-lowering effects in rats, showing low toxicity and potential for human trials.

    Area of Science:

    • Medicinal Chemistry
    • Pharmacology
    • Lipid Metabolism

    Background:

    • Probucol is a lipid-lowering drug with antioxidant properties.
    • Arylthioalkanoic acids represent a class of compounds with potential therapeutic applications.
    • Understanding structure-activity relationships is crucial for developing effective hypolipidemic agents.

    Purpose of the Study:

    • To synthesize and evaluate a series of arylthioalkanoic acids for hypolipidemic activity.
    • To identify optimal structural modifications for enhanced cholesterol and triglyceride reduction.
    • To assess the safety and efficacy of lead compounds.

    Main Methods:

    • Synthesis of novel arylthioalkanoic acid derivatives.
    • In vivo studies in rats to measure serum cholesterol and triglyceride levels.

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  • Toxicological assessment, including LD50 determination in mice.
  • Chiral resolution of active compounds.

    • Main Results:

    • Homologation of the alkyl side chain significantly impacted hypolipidemic activity, with compound 7 (2-[3,5-di-tert-butyl-4-hydroxyphenyl)thio]hexanoic acid) showing the best results.
    • Modifications to ring substitution did not improve activity.
    • Removal of the phenolic hydroxyl group in compound 23 retained similar activity to compound 7.
    • Replacing sulfur with oxygen increased toxicity.
    • Racemic compound 7 showed no difference in activity compared to resolved enantiomers.
    • Compound 7 exhibited low acute toxicity (LD50 between 5000-10000 mg/kg in mice).

    Conclusions:

    • Compound 7 is a potent hypolipidemic agent with a favorable safety profile.
    • The structure of compound 7, specifically the hexanoic acid chain, is critical for its activity.
    • Compound 7 warrants further investigation and has been advanced for human clinical evaluation.