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
Current Topics in Medicinal Chemistry
Title:Discovery and Optimization of Pyrazoline Derivatives As Promising Monoamine Oxidase Inhibitors
Volume: 12 Issue: 20
Author(s): Daniela Secci, Simone Carradori, Adriana Bolasco, Bruna Bizzarri, Melissa D’Ascenzio and Elias Maccioni
Affiliation:
Keywords: Alzheimer’s disease, antidepressant agents, isocarboxazid, monoamine oxidase, parkinson’s disease, pyrazoline
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.
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Secci Daniela, Carradori Simone, Bolasco Adriana, Bizzarri Bruna, D’Ascenzio Melissa and Maccioni Elias, Discovery and Optimization of Pyrazoline Derivatives As Promising Monoamine Oxidase Inhibitors, Current Topics in Medicinal Chemistry 2012; 12 (20) . https://dx.doi.org/10.2174/1568026611212200009
DOI https://dx.doi.org/10.2174/1568026611212200009 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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