title: Synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase A inhibitors.
abstract: New series of 4-methyl and 3,4-dimethyl-7-oxycoumarin derivatives (oxadiazoles, thiadiazoles, triazoles, and thiazolidinones) were designed, synthesized, and evaluated for their monoamine oxidase (MAO) A and B inhibiting effect. All the synthesized compounds showed in vitro high affinity and selectivity toward MAO-A isoenzyme, compared to clorgyline and moclobemide, with Ki values on the picomolar range. Moreover, most of the tested compounds displayed MAO inhibitory effect when tested in vivo. The docking experiments carried out on MAO-A and MAO-B structures proved new information about the enzyme-inhibitor interaction and the potential therapeutic application of 7-oxycoumarin scaffold.
authors.affiliation: Chemistry of Natural Products Department, National Research Center, Dokki, Egypt. ommryan@yahoo.com
authors.forename: Omaima M
authors.initials: OM
authors.lastname: Abdelhafez
authors.forename: Kamelia M
authors.initials: KM
authors.lastname: Amin
authors.forename: Hamed I
authors.initials: HI
authors.lastname: Ali
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Abdalla
authors.forename: Rasha Z
authors.initials: RZ
authors.lastname: Batran
mesh_terms: D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006860:Hydrogen Bonding; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008958:Models, Molecular; D008995:Monoamine Oxidase / Q000187:drug effects*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared
chemical_list: D003374:Coumarins; D008996:Monoamine Oxidase Inhibitors; D008995:Monoamine Oxidase