摘要
本文报道19个2(E)苯亚甲基环戊酮Mannich碱类化合物的合成。所有产物结构经元素分析、核磁共振氢谱和红外光谱证实。初步药理试验表明部分化合物有较强的抗炎活性。其中1个化合物对二甲苯致小鼠耳廓肿胀、角叉菜胶致大鼠足爪肿胀和乙酸致小鼠腹腔毛细血管通透性增加均有显著的抑制作用,抑制能力与布洛芬、阿斯匹林相近。
Nineteen kinds of 2(E)benzylidene5(Nsubstituted aminomethyl) cyclopentanones were synthesized via Mannich reaction or amine exchange reaction and identified spectrometrically. One compound exhibited significant antiinflammatory activity, showing obvious inhibitory effect on xyleneinduced mice ear swelling, carrageenininduced rats paw edema and increased capillary permeability induced with acetic acid in mice. Its ED50 values in these inflammatory models were calculated to be 678 mg·kg-1, 253 mg·kg-1 and 418 mg·kg-1 respectively, nearly equal to those of ibuprofen and aspirin.
出处
《药学学报》
CAS
CSCD
北大核心
1998年第5期344-349,共6页
Acta Pharmaceutica Sinica
关键词
抗炎药物
环戊酮
抗炎作用
Antiinflammatory agent
Cyclopentanone Mannich base
Amine exchange reaction