title: α-Ketoamino acid ester derivatives as promising MAO inhibitors.
abstract: α-Ketoamino acid ester 2-[2-(2-acetamidophenyl)-2-oxoacetamido] and 2-[4-(2-(2-acetamidophenyl)-2-oxoacetamido)benzamido] derivatives were synthesized via the ring opening of N-acetylisatin under mild conditions. These compounds were then examined for their capacity to inhibit monoamine oxidase (MAO). The inhibition profile was found to be competitive for compounds 4d, 6a, 6b and 6f, which showed MAO-A selectivity. Observation of the docked positions of these compounds revealed interactions with many residues previously reported to have an effect on the inhibition of the enzyme. Our findings indicate that the members of this family of α-ketoamino acid esters are promising MAO inhibitors.
authors.affiliation: Department of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia. aymanel_faham@hotmail.com
authors.forename: Ayman
authors.initials: A
authors.lastname: El-Faham
authors.lastname: Zainab Al Marhoon
authors.forename: Ahmed
authors.initials: A
authors.lastname: Abdel-Megeed
authors.forename: Sherine N
authors.initials: SN
authors.lastname: Khattab
authors.forename: Adnan A
authors.initials: AA
authors.lastname: Bekhit
authors.forename: Fernando
authors.initials: F
authors.lastname: Albericio
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis* / Q000378:metabolism; D000818:Animals; D004952:Esters; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis* / Q000378:metabolism; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism; D011485:Protein Binding / Q000502:physiology
chemical_list: D000596:Amino Acids; D004952:Esters; D007659:Ketones; D008996:Monoamine Oxidase Inhibitors