Depatment of Therapeutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt.
Eur J Med Chem. 2010 Jun;45(6):2117-31. doi: 10.1016/j.ejmech.2009.12.078. Epub 2010 Jan 21.
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.
已经合成了三系列螺环[(2H,3H)喹唑啉-2,1'-环己烷]-4(1H)-酮衍生物。一些新型的喹唑啉酮衍生物 IIe、VIIIc、XIc、XIIb、XIIc、XVIb 在实验大鼠中表现出相当强的抗炎和镇痛活性，且具有优于吲哚美辛和曲马多的胃肠道安全性。对具有最高抗炎活性的衍生物进行了 COX-2 的对接研究。化合物 XVIb 与吲哚美辛的 RMSD 值最接近。
