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  • Title: 2-(Aminomethyl)phenols, a new class of saluretic agents. 1. Effects of nuclear substitution.
    Author: Stokker GE, Deana AA, deSolms SJ, Schultz EM, Smith RL, Cragoe EJ, Baer JE, Ludden CT, Russo HF, Scriabine A, Sweet CS, Watson LS.
    Journal: J Med Chem; 1980 Dec; 23(12):1414-27. PubMed ID: 7452697.
    Abstract:
    A series of 2-(aminomethyl)phenols was synthesized and tested in rats and dogs for saluretic and diuretic activity. A number of these compounds exhibit a high order of activity on iv or po administration. The most active compounds belong to a subseries of 4-alkyl-6-halo derivatives of which 2, 2-(aminomethyl)-4-(1,1-dimethylethyl)-6-iodophenol, is the most active. Compound 2 also possesses significant antihypertensive activity, an adjunctive pharmacological parameter which distinguishes 2 from the other compounds prepared in this series. In addition, 2 displays both topical saluretic and antiinflammatory activities.
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