A number of bicyclic ring-fused analogues of 2-(aminomethyl)phenol were synthesized and tested orally in rats and intravenously in dogs for saluretic and diuretic effects. Of the 15 alicylic, aromatic, and heterocyclic ring-fused compounds tested, only 2-(aminomethyl)-4-chloro-1-naphthalenol hydrochloride (2) and 7-(aminomethyl)-6-hydroxy-5,8-dimethyl-1,2,3,4-tetrahydronaphthalene hydrochloride (6) displayed a high order of activity.

2-(aminomethyl)phenols show potential as a new class of saluretic agents, with 2-(aminomethyl)-4-chloro-1-naphthalenol hydrochloride showing high activity in rats and dogs.

Paper

2-(Aminomethyl)phenols, a new class of saluretic agents. 5. Fused-ring analogues.

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