【文章名】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
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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
作者
Amin, KM; Kamel, MM; Anwar, MM; Khedr, M; Syam, YM
[摘要]: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.