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Current Topics in Medicinal Chemistry

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ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

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Research Article

Thiazole-based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling

Author(s): Christophe Tratrat*, Michelyne Haroun, Evangelia Tsolaki, Anthi Petrou, Antonis Gavalas and Athina Geronikaki*

Volume 21, Issue 4, 2021

Published on: 14 December, 2020

Page: [257 - 268] Pages: 12

DOI: 10.2174/1568026621999201214232458

Price: $65

Abstract

Background: Inflammation is a multifactorial process reflecting the response of the organism to various stimuli and is associated with a number of disorders such as arthritis, asthma and psoriasis, which require long-lasting or repeated treatment.

Objective: The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chalcone derivatives.

Methods: Chalcones were synthesized via Cliazen-Schmidt condensation1-(4-methyl-2- alkylamino)thiazol-5-yl) ethanone with a corresponding aromatic aldehyde. For the evaluation of possible anti-inflammatory activity, carrageenan mouse paw edema was used.

Results: Eight out of thirteen tested chalcones showed anti-inflammatory activity in a range of 51- 55%. Prediction of toxicity revealed that these compounds are not toxic.

Conclusion: In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.

Keywords: Thiazole, Chalcone, NSAIDs, Toxicity, Docking, LOX.

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