SELECTIVE INHIBITORS OF MONOAMINE-OXIDASE .3. STRUCTURE-ACTIVITY RELATIONSHIP OF TRICYCLICS BEARING IMIDAZOLINE, OXADIAZOLE, OR TETRAZOLE GROUPS

Inhibition of monoamine oxidase A (MAO A) is believed to cause antidep ressant and possibly antianxiety effects. The previous paper had devel oped structure-activity relationships (SAR) for in vitro MAO A inhibit ion by tricyclic N-arylamides.(1) It is shown in this paper that the s ame in vitro SAR can be carried over to tricyclics whose potentially t oxic amide function is replaced by an appropriately substituted imidaz oline, 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 re versibility which correlates with a low ability to cause a blood press ure rise with ingested tyramine (''cheese effect'').