Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines
C Balakumar1, P Lamba, D Pran Kishore
1Centre with Potential for Excellence in Biomedical Sciences, Panjab University, Chandigarh 160 014, India.
European Journal of Medicinal Chemistry
|August 31, 2010
Abstract:
A series of novel 8/10-trifluoromethyl-substituted-imidazo[1,2-c] quinazolines have been synthesized and evaluated in vivo (rat paw edema) for their anti-inflammatory activity and in silico (docking studies) to recognize the hypothetical binding motif of the title compounds with the cyclooxygenase isoenzymes (COX-1 and COX-2) employing GOLD (CCDC, 4.0.1 version) software. The compounds, 9b and 10b, were found to have good anti-inflammatory activity [around 80% of the standard: indomethacin]. The binding mode of the title compounds has been proposed based on the docking studies.


