Thiazole-based Chalcone Derivatives as Potential Anti-inflammatory Agents: Biological Evaluation and Molecular Modelling.
Chalcone
Docking
LOX
NSAIDs
Thiazole
Toxicity
Journal
Current topics in medicinal chemistry
ISSN: 1873-4294
Titre abrégé: Curr Top Med Chem
Pays: United Arab Emirates
ID NLM: 101119673
Informations de publication
Date de publication:
2021
2021
Historique:
received:
28
09
2020
revised:
13
10
2020
accepted:
16
11
2020
pubmed:
16
12
2020
medline:
13
7
2021
entrez:
15
12
2020
Statut:
ppublish
Résumé
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. The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chalcone derivatives. 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. 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. In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.
Sections du résumé
BACKGROUND
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
OBJECTIVE
The aim of this paper is to evaluate the anti-inflammatory activity of previous synthesized thiazole-based chalcone derivatives.
METHODS
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
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
CONCLUSIONS
In general, it can be concluded that these compounds can be used for further modifications in order to develop more active and safe agents.
Identifiants
pubmed: 33319674
pii: CTMC-EPUB-112432
doi: 10.2174/1568026621999201214232458
doi:
Substances chimiques
Anti-Inflammatory Agents
0
Chalcones
0
Thiazoles
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
257-268Informations de copyright
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