新型苯并咪唑衍生物的体内镇痛和抗炎活性。
In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives.
机构信息
P. G. Department of Studies in Chemistry, Karnatak University, Pavate Nagar, Dharwad, Karnataka 580 003, India.
出版信息
Eur J Med Chem. 2010 May;45(5):2048-54. doi: 10.1016/j.ejmech.2010.01.029. Epub 2010 Jan 21.
A series of 2-methylaminobenzimidazole derivatives (1-11) were synthesized by the reaction of 2-(chloromethyl)-1H-benzimidazole derivatives with primary aromatic amines. All these compounds were characterized by IR, 1H NMR, 13C NMR, GC-MS and elemental analysis. The newly synthesized compounds were screened for analgesic and anti-inflammatory activities on acetic acid induced writhing in mice and carrageenan induced paw oedema in rats. Compounds (7) and (2) showed a potent analgesic (89% at 100 mg/kg b.w) and anti-inflammatory (100% at 100 mg/kg b.w) activities compared with standard drug Nimesulide (100% at 50 mg/kg b.w) respectively. The other compounds showed good analgesic and anti-inflammatory activities.
一系列 2-甲基氨基苯并咪唑衍生物（1-11）是通过 2-（氯甲基）-1H-苯并咪唑衍生物与伯芳胺反应合成的。所有这些化合物均通过 IR、1H NMR、13C NMR、GC-MS 和元素分析进行了表征。新合成的化合物在醋酸诱导的小鼠扭体反应和角叉菜胶诱导的大鼠足肿胀模型中进行了镇痛和抗炎活性筛选。化合物（7）和（2）分别显示出很强的镇痛（100mg/kg b.w 时为 89%）和抗炎（100mg/kg b.w 时为 100%）活性，与标准药物尼美舒利（50mg/kg b.w 时为 100%）相比。其他化合物也表现出良好的镇痛和抗炎活性。
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