Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines.
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.
Balakumar
C
C
Centre with Potential for Excellence in Biomedical Sciences, Panjab University, Chandigarh 160 014, India.
Lamba
P
P
Kishore
D Pran
DP
Narayana
B Lakshmi
BL
Rao
K Venkat
KV
Rajwinder
K
K
Rao
A Raghuram
AR
Shireesha
B
B
Narsaiah
B
B
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D005260:Female; D005461:Fluorine / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar
D000893:Anti-Inflammatory Agents; D011799:Quinazolines; D005461:Fluorine