Pyrazoline: A Promising Scaffold for the Inhibition of Monoamine Oxidase

ISSN: 1875-6166 (Online)
ISSN: 1871-5249 (Print)


Volume 14, 2 Issues, 2014


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Central Nervous System Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Gregory S. Hamilton
Eisai Inc.
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Pyrazoline: A Promising Scaffold for the Inhibition of Monoamine Oxidase

Author(s): Bijo Mathew, Jerad Suresh, Sockalingam Anbazhagan and Githa Elizabeth Mathew

Affiliation: Department of Pharmaceutical Chemistry Grace College of Pharmacy, Palakkad 678004, Kerala, India.

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.

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Article Details

Volume: 13
Issue Number: 3
First Page: 195
Last Page: 206
Page Count: 12
DOI: 10.2174/1871524914666140129122632
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