title: Selective inhibitors of monoamine oxidase. 3. Structure-activity relationship of tricyclics bearing imidazoline, oxadiazole, or tetrazole groups.
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.  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").
authors.affiliation: Division of Organic Chemistry, Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709, USA.
authors.forename: M
authors.initials: M
authors.lastname: Harfenist
authors.forename: D J
authors.initials: DJ
authors.lastname: Heuser
authors.forename: C T
authors.initials: CT
authors.lastname: Joyner
authors.forename: J F
authors.initials: JF
authors.lastname: Batchelor
authors.forename: H L
authors.initials: HL
authors.lastname: White
mesh_terms: D007093:Imidazoles / Q000032:analysis*; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D010069:Oxadiazoles / Q000032:analysis*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000032:analysis*
chemical_list: D007093:Imidazoles; D008996:Monoamine Oxidase Inhibitors; D010069:Oxadiazoles; D013777:Tetrazoles