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Structure activity correlation for diuretic furosemide congeners.

J Shani, S Schoenberg, E J Lien

    Pharmacology
    |January 1, 1983
    PubMed
    Summary
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    This study explored anthranilic acid derivatives for diuretic and saluretic effects. Increased lipophilicity (log P) positively impacts diuretic activity, but only up to a certain limit.

    Area of Science:

    • Medicinal Chemistry
    • Pharmacology

    Background:

    • Anthranilic acid derivatives are a class of compounds with potential biological activities.
    • Understanding structure-activity relationships is crucial for drug design.

    Purpose of the Study:

    • To investigate the structure-activity correlation of anthranilic acid derivatives.
    • To evaluate the diuretic and saluretic activities of synthesized compounds.

    Main Methods:

    • Synthesis of 59 anthranilic acid derivatives.
    • Testing compounds for diuretic and saluretic activities.
    • Correlating biological activity with physicochemical constants, including log P.

    Main Results:

    • A positive correlation was found between diuretic activity and lipophilicity (log P).

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  • The lipophilicity of the molecule primarily governs biological activity within a specific range.
  • Further increases in log P did not enhance diuretic activity.

    • Conclusions:

    • Lipophilicity is a key determinant of diuretic activity for these anthranilic acid derivatives.
    • Optimal lipophilicity exists for maximizing diuretic effects, beyond which activity plateaus.