Synthesis, biological evaluation and molecular docking of novel series of spiro [(2H,3H) quinazoline-2,1'- cyclohexan]-4(1H)- one derivatives as anti-inflammatory and analgesic agents
- PMID: 20137837
- DOI: 10.1016/j.ejmech.2009.12.078
Synthesis, biological evaluation and molecular docking of novel series of spiro [(2H,3H) quinazoline-2,1'- cyclohexan]-4(1H)- one derivatives as anti-inflammatory and analgesic agents
Abstract
Three series of Spiro [(2H,3H) quinazoline-2,1'-cyclohexan]-4(1H)-one derivatives have been synthesized. Some of the novel quinazolinone derivatives IIe, VIIIc, XIc, XIIb, XIIc, XVIb showed considerable potent anti-inflammatory and analgesic activity of superior G.I.T. safety profile in experimental rats in comparing to indomethacin and tramadol as reference drugs. Docking study into COX-2 has been made for derivatives of highest anti-inflammatory activity. The compound XVIb showed the nearest RMSD value to that of indomethacin.
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