2-(Aminomethyl)phenols, a new class of saluretic agents. I. Effect of nuclear substitution

Article abstract of DOI:10.1021/jm00186a024

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-iodophenyl, 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.