Synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase A inhibitors. Academic Article

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

• Ali, Hamed

published proceedings

• J Med Chem

author list (cited authors)

• Abdelhafez, O. M., Amin, K. M., Ali, H. I., Abdalla, M. M., & Batran, R. Z.

citation count

• 33

complete list of authors

• Abdelhafez, Omaima M||Amin, Kamelia M||Ali, Hamed I||Abdalla, Mohamed M||Batran, Rasha Z

publication date

• December 2012

publisher

• American Chemical Society (ACS)  Publisher

published in

• Journal of Medicinal Chemistry  Journal

keywords

• Coumarins
• Hydrogen Bonding
• MONOAMINE OXIDASE
• Magnetic Resonance Spectroscopy
• Mass Spectrometry
• Models, Molecular
• Monoamine Oxidase Inhibitors
• Spectrophotometry, Infrared

PubMed Central ID

• 23153282

Digital Object Identifier (DOI)

• 10.1021/jm301014y

start page

• 10424

end page

• 10436

volume

• 55

issue

• 23

URL

• http://dx.doi.org/10.1021/jm301014y