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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5230
ISSN (Online): 1875-614X

Research Article

Pyrazoles as Anti-inflammatory and Analgesic Agents: In-vivo and In-silico Studies

Author(s): Geeta Chahal, Jyoti Monga, Isha Rani, Shubham Saini, Manish Devgun, Asif Husain and Sukhbir Lal Khokra*

Volume 23, Issue 1, 2024

Published on: 12 December, 2023

Page: [39 - 51] Pages: 13

DOI: 10.2174/0118715230275741231207115011

Price: $65

Abstract

Background: Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There are well-known marketed drugs having pyrazole moiety as celecoxib, and lonazolac as COX-II inhibitors.

Aims: We aim to synthesize better anti-inflammatory than existing ones. Thiophene is also known for its analgesic and anti-inflammatory action. Thus, the fusion of both gives better anti-inflammatory agents. In the present studies, derivatives from two series of pyrazole were prepared by reacting substituted chalcone (3a-3f) derivatives prepared from 2-acetyl thiophene. They substituted aromatic aldehydes with phenyl hydrazine to form (5a-5f) and with 2, 4-dinitro phenyl hydrazine giving compounds (6a-6f) separately.

Methods: Purified and characterized pyrazoles have been analyzed for in-vivo analgesic and anti-inflammatory activities by using standard methods. Compounds 5e, 5f, and 6d were proved to be potent analgesics and series (5a-5f) was found to have anti-inflammatory action, which was further validated using docking and ADME studies.

Results: The ADME profile of synthesized compounds was found to be satisfactory.

Conclusion: The synthesized compounds can serve as lead for further drug designing.

Keywords: Docking, molegro virtual docker, swiss adme, pyrazole, anti-inflammatory, analgesic.

Graphical Abstract
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