4.7 Article

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 45, Issue 6, Pages 2117-2131

Publisher

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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