| 四氢苯并咪唑类衍生物的合成及其环氧合酶-2抑制活性 |
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| 引用本文： | 李美英,刘河,仲伯华.四氢苯并咪唑类衍生物的合成及其环氧合酶-2抑制活性[J].中国药物化学杂志,2006,16(5):284-288. |
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| 作者姓名： | 李美英 刘河 仲伯华 |
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| 作者单位： | 军事医学科学院,毒物药物研究所,北京,100850 |
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| 摘 要： | 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.
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| 关 键 词： | 药物化学 化合物制备 化学合成 COX-2选择性抑制剂 四氢苯并咪唑类衍生物 |
| 文章编号： | 1005-0108（2006）05-0284-05 |
| 收稿时间： | 2006-04-30 |
| 修稿时间： | 2006年4月30日 |
Synthesis and COX-2 inhibitory activities of 1,2-bisaryl tetrahydrobenzimidazoles |
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| LI Mei-ying,LIU He,ZHONG Bo-hua.Synthesis and COX-2 inhibitory activities of 1,2-bisaryl tetrahydrobenzimidazoles[J].Chinese Journal of Medicinal Chemistry,2006,16(5):284-288. |
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| Authors: | LI Mei-ying LIU He ZHONG Bo-hua |
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| Institution: | Institute of Pharmacology and Toxicology, Academy of Military Medicinal Science, Beijing 100850, China |
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| Abstract: | Aim To find potent and selective cyclooxygenase-2(COX-2) inhibitors 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 tetrahydrobenzimidazoles were prepared.Their chemical structures were confirmed by elemental analysis,()~1H-NMR,()~(13)C-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. |
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| Keywords: | medicinal chemistry compound preparation chemical synthesis COX-2 selective inhibitors tetrahydrobenzimidazole derivatives |
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