title: Discovery and optimization of pyrazoline derivatives as promising monoamine oxidase inhibitors.
abstract: Among different heterocyclic chemotypes incorporating two nitrogen atoms, pyrazolines could be considered a valid pharmacophore for the synthesis of selective monoamine oxidase (MAO) inhibitors because they were developed by the cyclization of the early hydrazine derivatives such as isocarboxazid. Substituted pyrazolines, decorated with different functional groups, are important lead compounds endowed with a large amount of biological activities. As a matter of this, most of them were also evaluated as dual inhibitors with a synergistic action towards different classes of enzymes (ciclooxygenase, acetylcholinesterase, butyrylcholinesterase). Moreover due to the direct correlation with the recognized MAO inhibition, this scaffold displayed antidepressant and anticonvulsant properties in animal models.
authors.affiliation: Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy. daniela.secci@uniroma1.it
authors.forename: Daniela
authors.initials: D
authors.lastname: Secci
authors.forename: Simone
authors.initials: S
authors.lastname: Carradori
authors.forename: Adriana
authors.initials: A
authors.lastname: Bolasco
authors.forename: Bruna
authors.initials: B
authors.lastname: Bizzarri
authors.forename: Melissa
authors.initials: M
authors.lastname: D'Ascenzio
authors.forename: Elias
authors.initials: E
authors.lastname: Maccioni
mesh_terms: D000818:Animals; D006801:Humans; D008958:Models, Molecular; D056004:Molecular Dynamics Simulation; D008995:Monoamine Oxidase / Q000737:chemistry / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D019636:Neurodegenerative Diseases / Q000188:drug therapy* / Q000201:enzymology; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship
chemical_list: D008996:Monoamine Oxidase Inhibitors; D011720:Pyrazoles; D008995:Monoamine Oxidase