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

Curr Top Med Chem. 2021;21(4):257-268. doi: 10.2174/1568026621999201214232458.

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: Chalcone; Docking; LOX; NSAIDs; Thiazole; Toxicity.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemistry
  • Anti-Inflammatory Agents / pharmacology*
  • Anti-Inflammatory Agents / therapeutic use
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Chalcones / therapeutic use
  • Inflammation / drug therapy
  • Mice
  • Models, Molecular*
  • Molecular Docking Simulation
  • Thiazoles / chemistry*

Substances

  • Anti-Inflammatory Agents
  • Chalcones
  • Thiazoles