Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 6, Pages 2117-2131Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2009.12.078
Keywords
Spiro [(2H,3H) quinazoline-2,1 '-cyclohexan]-4(1H)-one; Antinflammatory; Analgesic; Ulcerogenic effect; Molecular docking; Cyclooxygenase-2
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Three series of Spiro 1(2H,3H) quinazoline-2,1'-cyclohexan1-4(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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