Journal of Medicinal Chemistry p. 1414 - 1427 (1980)
Update date:2022-08-05
Topics:
Stokker
Deana
deSolms
Schultz
Smith
Cragoe Jr.
Baer
Ludden
Russo
Scriabine
Sweet
Watson
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.
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