Selective Inhibitors of Monoamine Oxidase. 3. Structure−Activity Relationship of Tricyclics Bearing Imidazoline, Oxadiazole, or Tetrazole Groups

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Abstract
Inhibition of monoamine oxidase A (MAO A) is believed to cause antidepressant and possibly antianxiety effects. The previous paper had developed structure−activity relationships (SAR) for in vitro MAO A inhibition by tricyclic N-arylamides.l It is shown in this paper that the same in vitro SAR can be carried over to tricyclics whose potentially toxic amide function is replaced by an appropriately substituted imidazoline, a 1,2,4- or 1,3,4-oxadiazole, or an alkylated tetrazole moiety. Dialysis of the inhibitor from the enzyme was used as a measure of reversibility which correlates with a low ability to cause a blood pressure rise with ingested tyramine (“cheese effect”).