Title of article :
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
Author/Authors :
Haider, Saqlain Department of Chemistry, Faculty of Science - Jamia Hamdard (Hamdard University) New Delhi -110 062, India , Sarwar Alam, Mohammad Department of Chemistry, Faculty of Science - Jamia Hamdard (Hamdard University) New Delhi -110 062, India , Hamid, Hinna Department of Chemistry, Faculty of Science - Jamia Hamdard (Hamdard University) New Delhi -110 062, India , Umar, Sadiq Department of Toxicology - Faculty of Science - Jamia Hamdard(Hamdard University) New Delhi -110062, India , Kumar, Deepak Department of Pharmaceutical Chemistry - Sikkim Central University, Sikkim-737136, India , Nazreen, Syed Department of Chemistry, Faculty of Science - Jamia Hamdard (Hamdard University) New Delhi -110 062, India
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.
Keywords :
Arthritis , Glutathione , Tnf-α , Cox-2 Selectivity , Prostaglandins
