title: Thiazole derivatives as inhibitors of purified bovine liver mitochondrial monoamine oxidase-B: structure-activity relationships and theoretical study.
abstract: Structure-activity relationships were performed on a new series of thiazole derivatives which selectively inactivate monoamine oxidase-B (MAO-B), purified from mitochondrial beef liver. All of the synthesized and tested compounds showed non-competitive inhibition, suggesting the formation of a stable adduct between the tertiary amine function, linked to the thiazolyl derivatives and the active site of the enzyme. The mechanism of MAO-B inhibition is discussed in terms of the Ionization Potential of the amine nitrogen atom and the conformational flexibility of the inhibitors.
authors.affiliation: Istituto di Scienze Biochimiche e Farmacologiche, University of Catania, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Cambria
authors.forename: A
authors.initials: A
authors.lastname: Raudino
authors.forename: A
authors.initials: A
authors.lastname: Geronikaki
authors.forename: G
authors.initials: G
authors.lastname: Buemi
authors.forename: G
authors.initials: G
authors.lastname: Raciti
authors.forename: P
authors.initials: P
authors.lastname: Mazzone
authors.forename: S
authors.initials: S
authors.lastname: Guccione
authors.forename: S
authors.initials: S
authors.lastname: Ragusa
mesh_terms: D000818:Animals; D020134:Catalytic Domain / Q000187:drug effects; D002417:Cattle; D008930:Mitochondria, Liver / Q000201:enzymology*; D008962:Models, Theoretical; D008968:Molecular Conformation; D008995:Monoamine Oxidase / Q000187:drug effects*; D008996:Monoamine Oxidase Inhibitors / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
chemical_list: D008996:Monoamine Oxidase Inhibitors; D013844:Thiazoles; D008995:Monoamine Oxidase