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


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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 moi-ety 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.

About the authors

Geeta Chahal

Institute of Pharmaceutical Sciences, Kurukshetra University

Email: info@benthamscience.net

Jyoti Monga

, Ch. Devi Lal College of Pharmacy

Email: info@benthamscience.net

Isha Rani

, Spurthy College of Pharmacy

Email: info@benthamscience.net

Shubham Saini

Institute of Pharmaceutical Sciences, Kurukshetra University

Email: info@benthamscience.net

Manish Devgun

Institute of Pharmaceutical Sciences, Kurukshetra University

Email: info@benthamscience.net

Asif Husain

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research,, Jamia Hamdard

Email: info@benthamscience.net

Sukhbir Lal Khokra

Institute of Pharmaceutical Sciences, Kurukshetra University

Author for correspondence.
Email: info@benthamscience.net

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