2-(E)-苯亚甲基-5-(N-取代胺甲基)环戊酮的合成及抗炎作用  

SYNTHESIS AND ANTIINFLAMMATORY ACTIVITY OF 2(E)BENZYLIDENE5(NSUBSTITUTEDAMINOMETHYL) CYCLOPENTANONES

作　　者：董金华[1] 徐莉英[1] 秦华[1] 陈思维[1] 计志忠[1] 王敏伟[1] 

机构地区：[1]沈阳药科大学

出　　处：《药学学报》1998年第5期344-349,共6页Acta Pharmaceutica Sinica

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)benzylidene5(Nsubstituted 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 xyleneinduced mice ear swelling, carrageenininduced rats paw edema and increased capillary permeability induced with acetic acid in mice. Its ED50 values in these inflammatory models were calculated to be 678 mg·kg-1, 253 mg·kg-1 and 418 mg·kg-1 respectively, nearly equal to those of ibuprofen and aspirin.

关 键 词：抗炎药物 环戊酮 抗炎作用 

分 类 号：TQ463.53[化学工程—制药化工] R971.1[医药卫生—药品]