Synthesis and Evaluation of Novel 2-Substituted-quinazolin-4(3<i>H</i>)-ones as Potent Analgesic and Anti-inflammatory Agents
作者:Bilal Ahmad Rather、Tilak Raj、Aravind Reddy、Mohan Paul S. Ishar、Samitha Sivakumar、Perumal Paneerselvam
DOI:10.1002/ardp.200900231
日期:2010.1.27
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
通过将 3,5-二取代-邻氨基苯甲酸与乙酸酐/苯甲酰氯反应合成一系列新型 2-取代-喹唑啉-4(3H)-酮,再与不同的伯胺反应得到 2,6,8 -取代的喹唑啉-4(3H)-ones 6a-f, 7, 8. 对所有合成的化合物进行表征并筛选其镇痛和抗炎活性。化合物 6,8-二溴-2-苯基-3-(4'-羧基苯基)喹唑啉-4(3H)-one 7 和 6,8-二溴-2-苯基-3-(2'-苯基乙酸)喹唑啉‐4(3H)-one 8 分别与参考标准乙酰水杨酸和吲哚美辛相比显示出良好的镇痛和抗炎活性。