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
Conclusion: From results, it was observed that highly substituted thiophene scaffold exhibits
anti-inflammatory and antioxidant activity.