Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, Punjab, India.
Arch Pharm (Weinheim). 2010 Feb;343(2):108-13. doi: 10.1002/ardp.200900231.
A novel series of 2-substituted-quinazolin-4(3H)-ones were synthesized by reacting 3,5-disubstituted-anthranilic acid with acetic anhydride/benzoyl chloride, which were further reacted with different primary amines to obtain 2,6,8-substituted-quinazolin-4(3H)-ones 6a-f, 7, 8. All the synthesized compounds were characterized and screened for analgesic and anti-inflammatory activities. Compounds 6,8-dibromo-2-phenyl-3-(4'-carboxyl phenyl)quinazolin-4(3H)-one 7 and 6,8-dibromo-2-phenyl-3-(2'-phenylethanoic acid)quinazolin-4(3H)-one 8 displayed good analgesic and anti-inflammatory activity in comparison to the reference standards acetyl salicylic acid and indomethacin, respectively.
通过将 3,5-二取代邻氨基苯甲酸与乙酸酐/苯甲酰氯反应，合成了一系列新型 2-取代-4(3H)-喹唑啉酮。然后，这些化合物与不同的伯胺进一步反应，得到了 2,6,8-取代-4(3H)-喹唑啉酮 6a-f、7 和 8。所有合成的化合物均经过了表征，并对其进行了镇痛和抗炎活性筛选。与对照标准乙酰水杨酸和吲哚美辛相比，化合物 6,8-二溴-2-苯基-3-(4'-羧基苯基)喹唑啉-4(3H)-酮 7 和 6,8-二溴-2-苯基-3-(2'-苯乙 酸)喹唑啉-4(3H)-酮 8 表现出良好的镇痛和抗炎活性。
