Discovery and Optimization of Pyrazoline Derivatives As Promising Monoamine Oxidase Inhibitors

Author(s): Daniela Secci, Simone Carradori, Adriana Bolasco, Bruna Bizzarri, Melissa D’Ascenzio, Elias Maccioni

Journal Name: Current Topics in Medicinal Chemistry

Volume 12 , Issue 20 , 2012

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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.

Keywords: Alzheimer’s disease, antidepressant agents, isocarboxazid, monoamine oxidase, parkinson’s disease, pyrazoline

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Article Details

VOLUME: 12
ISSUE: 20
Year: 2012
Published on: 06 February, 2013
Page: [2240 - 2257]
Pages: 18
DOI: 10.2174/1568026611212200009
Price: $65

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