Abstract
In the five membered nitrogen containing heterocyclic family, pyrazoline could be recognized as a promising scaffold for the inhibition of Monoamine oxidase. Substitution at 1, 3 and 5-position of the pyrazoline nucleus displayed a significant activity towards MAO in the past 15 years. Our study identified the detailed structure activity relationship, the structural requirement for enzyme interaction and the effect of chirality on the pyrazoline nucleus towards MAO-A and MAO-B. We propose that the selectivity of pyrazoline nucleus towards MAO isoenzyme depends up on the bulkiness of the ring in the 1 and 3 position of the scaffold. The current review revealed that the derivatives of pyrazolines have proven to be versatile pharmacophores for the inhibition of MAO on the basis of existing literatures between (1998-2013).
Keywords: Anti-depressant, MAO-A, MAO-B, chirality, molecular docking.
Central Nervous System Agents in Medicinal Chemistry
Title:Pyrazoline: A Promising Scaffold for the Inhibition of Monoamine Oxidase
Volume: 13 Issue: 3
Author(s): Bijo Mathew, Jerad Suresh, Sockalingam Anbazhagan and Githa Elizabeth Mathew
Affiliation:
Keywords: Anti-depressant, MAO-A, MAO-B, chirality, molecular docking.
Abstract: In the five membered nitrogen containing heterocyclic family, pyrazoline could be recognized as a promising scaffold for the inhibition of Monoamine oxidase. Substitution at 1, 3 and 5-position of the pyrazoline nucleus displayed a significant activity towards MAO in the past 15 years. Our study identified the detailed structure activity relationship, the structural requirement for enzyme interaction and the effect of chirality on the pyrazoline nucleus towards MAO-A and MAO-B. We propose that the selectivity of pyrazoline nucleus towards MAO isoenzyme depends up on the bulkiness of the ring in the 1 and 3 position of the scaffold. The current review revealed that the derivatives of pyrazolines have proven to be versatile pharmacophores for the inhibition of MAO on the basis of existing literatures between (1998-2013).
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Cite this article as:
Mathew Bijo, Suresh Jerad, Anbazhagan Sockalingam and Mathew Elizabeth Githa, Pyrazoline: A Promising Scaffold for the Inhibition of Monoamine Oxidase, Central Nervous System Agents in Medicinal Chemistry 2013; 13 (3) . https://dx.doi.org/10.2174/1871524914666140129122632
DOI https://dx.doi.org/10.2174/1871524914666140129122632 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
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