Synthesis of Novel Amide Containing Schiffs Bases of 5-(4- Chloro-Phenyl)-Furan-2-Carboxaldehyde: Their In Vivo Anti- Inflammatory, Antioxidant and Antinociceptive Activities with Ulcerogenic Risk Evaluation

Abstract

A library of eighteen amide containing Schiffs bases has been synthesized and screened for their anti-inflammatory, antioxidant and antinociceptive activities. The compound 2 (COX-1 IC50 = 63.23 μM; COX-2 IC50 = 1.80 μM; SI = 35.12) exhibited potent selective COX-2 inhibition as compared to indomethacin (COX-1 IC50 = 3.60 μM; COX-2 IC50 = 7.50 μM; SI = 0.48). The compounds 2 and 7 reduced the COX-2 level to 7.5 ±0.35 nmole/min/ml and 6.8 ± 0.32nmole/min/ml respectively. The compounds 6 exhibited reduced the TNF-α level to 3.36 ± 0.18pg/ml. The compounds 2, 6, 7, 13 and 17 did not induce any gastric ulceration in comparison to the standard drug indomethacin.