摘要
目的研究 (1H) 3,4 二氢吡咯 [2 ,1 c][1,4 ]嗪 1 酮 (Ⅲ )类化合物抗炎镇痛作用的构效关系。方法通过 2 吡咯甲酸甲酯与 1,2 二溴乙烷N 烃基化反应 ,制得 1 (2 溴乙基 )吡咯 2 甲酸甲酯 (Ⅳ ) ,经过氧化银处理 ,得到Ⅲ ;通过Friedel Crafts酰基化反应 ,合成Ⅲ的 6 酰基衍生物Ⅴ1～Ⅴ8;用小鼠测试了所合成的化合物的抗炎镇痛活性。结果与结论合成了 8个目标化合物 ;药理实验表明 ,所合成的一些化合物具有明显的抗炎和 /或镇痛活性 ,其中Ⅴ5活性最强。
Aim To study the structure activity relationships(SAR)of the title compounds and search for new anti inflammatory and analgesic agents.Methods (1 H ) 3,4 dihydropyrrolooxazin 1 one(Ⅲ)was prepared from methyl 2 pyrrolecarboxylate by the N alkylation of 1,2 dibromoethane,and treatment of methyl 1 (2 bromoethyl)pyrrole 2 carboxylate(Ⅳ)with silver oxide.The Friedel Crafts reaction of Ⅲ with acyl chloride afforded the 6 acyl derivatives(Ⅴ 1～Ⅴ 8).The anti inflammatory and analgesic activities were tested in mice.Results and Conclusion Eight of 6 acyl 3,4 dihydropyrrolo oxazin 1 ones were synthesized.Most of the compounds showed remarkable anti inflammatory and/or analgesic activities in mice.The compound Ⅴ 5 showed the most potent anti inflammatory and analgesic activities.
出处
《中国药物化学杂志》
CAS
CSCD
2002年第6期329-332,共4页
Chinese Journal of Medicinal Chemistry
