Thiazole-based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling-Reference-Cited by-同舟云学术

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

Published:2021-04 Issue:4 Volume:21 Page:257-268
ISSN:1568-0266
Container-title:Current Topics in Medicinal Chemistry
language:en
Short-container-title:CTMC

Author:

Tratrat Christophe¹,Haroun Michelyne¹,Tsolaki Evangelia²,Petrou Anthi³,Gavalas Antonis³,Geronikaki Athina³

Affiliation:

1. Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982,Saudi Arabia

2. School of Chemical and Bioprocess Engineering, University College Dublin,Ireland

3. Aristotle University of Thessaloniki, School of Pharmacy, Thessaloniki 54124,Greece

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.

Funder

Deputy ship for Research & Innovation, Ministry of Education in Saudi Arabia

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,General Medicine

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