Synthesis and Biological Evaluation of Novel 2-(4-acetyl-3-methyl- 5-(arylamino) thiophen-2-yl)-3-arylquinazolin-4(3H)-one Derivatives as Potential Anti-inflammatory and Antioxidant Agents.
Antiinflamm Antiallergy Agents Med Chem
; 17(2): 102-114, 2018.
Article
en En
| MEDLINE
| ID: mdl-30198442
ABSTRACT
BACKGROUND:
A new series of 2-(4-acetyl-3-methyl-5-(arylamino) thiophen-2- yl)-3-arylquinazolin-4(3H)-one derivatives (11a-11j) were synthesized from acetyl acetone, phenyl isothiocyanate and 2-chloromethyl quinazolinone.OBJECTIVE:
Due to side effects of Non Steroidal Anti-Inflammatory Drugs (NSAID), an attempt was made to identify the novel tetrasubstituted thiophene lead compound as potential anti-inflammatory and antioxidant agent.METHODS:
Then newly synthesized compounds were characterized by IR spectroscopy, 1H NMR and mass spectrometry. The synthesized compounds were screened for their in vivo anti-inflammatory activity in carrageenan-induced rat hind paw edema model at dose 20mg/kg body weight using diclofenac sodium as a standard drug. The compounds were also evaluated for their in vitro DPPH free radical-scavenging activity and nitric oxide radical scavenging activity at the concentrations of 10, 20, 40, 60, 80 and 100 µg/mL using ascorbic acid as standard drug.RESULTS:
The results from carrageenan-induced rat hind paw edema showed that compounds 11e, 11f and 11b show a significant anti-inflammatory activity of 46.61%, 48.94% and 47.04 % protection respectively to inflamed paw but less than diclofenac sodium. Compounds 11h and 11e show good DPPH free radical scavenging and nitric oxide radical scavenging activity, respectively.CONCLUSION:
From results, it was observed that highly substituted thiophene scaffold exhibits anti-inflammatory and antioxidant activity.Palabras clave
Texto completo:
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Banco de datos:
MEDLINE
Asunto principal:
Quinazolinas
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Tiofenos
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Depuradores de Radicales Libres
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Edema
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Antiinflamatorios
Límite:
Animals
Idioma:
En
Año:
2018
Tipo del documento:
Article