2-(Aminomethyl)phenols, a new class of saluretic agents. 1. Effects of nuclear substitution.
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.
D000284:Administration, Oral; D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D004232:Diuretics / Q000008:administration & dosage / Q000138:chemical synthesis*; D004285:Dogs; D005260:Female; D007275:Injections, Intravenous; D009318:Natriuresis / Q000187:drug effects*; D010636:Phenols / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D004232:Diuretics; D010636:Phenols