四氢苯并咪唑类衍生物的合成及其环氧合酶-2抑制活性

Synthesis and COX-2 inhibitory activities of 1,2-bisaryl tetrahydrobenzimidazoles

目的寻找新型不良反应小的环氧合酶-2(COX-2)选择性抑制剂。方法结合典型COX-2选择性抑制剂基本结构特征,设计并合成一系列新型四氢苯并咪唑类化合物。采用化学发光法测试化合物对环氧合酶-2的抑制活性。结果与结论设计并合成了13个新型四氢苯并咪唑类化合物,其结构经元素分析、1H-NMR、13C-NMR和MS确证,所有化合物均未见文献报道。部分化合物对环氧合酶-2的抑制活性结果表明,化合物1、3、6对COX-2有一定的抑制作用。

Aim To find potent and selective cyclooxygenase-2 （COX-2） inhlbitors with safer profile. Methods A series of novel N-aryl-2-substituted tetrahydrobenzimidazoles containing a methylsulphonyl group in the para-position of N-aromatic ring were designed and synthesized. The COX-2 inhibitory activities of these compounds were investigated by chemiluminescent COX inhibitor screening assay. Result and conclusion Thirteen novel N-arylation-2-substituted tetrahydrobenzlmidazoles were prepared. Their chemical structures were confirmed by elemental analysis, ^1H-NMR, ^13C-NMR and MS. None of them has been reported yet. Test on the COX-2 inhibitory activities of some compounds show that they have inhibitory activities on COX-2.