Synthesis, anti-inflammatory evaluation and docking studies of some new fluorinated fused quinazolines.

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.

• Authors: C Balakumar, P Lamba, D Pran Kishore, B Lakshmi Narayana, K Venkat Rao, K Rajwinder, A Raghuram Rao, B Shireesha, B Narsaiah
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 45 Issue 11 Pg. 4904-13 (Nov 2010) ISSN: 1768-3254 [Electronic] France
• PMID: 20800934 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Crown Copyright © 2010. Published by Elsevier Masson SAS. All rights reserved.

Chemical References

• Anti-Inflammatory Agents
• Quinazolines
• Fluorine

Topics

• Animals
• Anti-Inflammatory Agents (chemical synthesis, pharmacology)
• Drug Evaluation, Preclinical
• Female
• Fluorine (chemistry)
• Magnetic Resonance Spectroscopy
• Models, Molecular
• Quinazolines (chemical synthesis, pharmacology)
• Rats
• Rats, Wistar