| 新型苯并咪唑类人顶体酶抑制剂的设计、合成及活性研究 |
| 投稿时间：2012-02-13 修订日期：2012-03-27 点此下载全文 |
| 引用本文：樊永正,陈倩倩,刘伯石,赵军涛,田巍,周有骏,吕加国,朱驹.新型苯并咪唑类人顶体酶抑制剂的设计、合成及活性研究[J].药学实践杂志,2012,30(3):203~206,210 |
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| 中文摘要:目的 基于人精子顶体酶活性位点的三维结构设计并合成新型苯并咪唑类衍生物。 方法 计算机模拟设计及化学合成。 结果 设计并合成了10个苯并咪唑类化合物,进行了抑酶活性测试。 结论 所有合成的化合物具有较好的抑酶活性,其中化合物8a是对照物Nα-对甲苯磺酰-L-赖氨酸氯甲基酮(TLCK)的1426倍。 |
| 中文关键词:精子顶体酶 抑制剂 设计 合成 抑酶活性 苯并咪唑 |
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| Synthesis and effect of novel 1-(1H-benzimidazole-2-yl) -urea derivatives as human acrosin inhibitors |
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| Abstract:Objective To design and synthesize novel 1-(1H-benzimidazole-2-yl)urea compounds on the basis of the active site of human acrosin. Methods The compounds were designed by computer modeling and synthesized. Results Ten 1-(1H-benzimidazole-2-yl)urea compounds were designed and synthesized, in vitro anti-acrosin activity were tested. Conclusions The results of in vitro anti-acrosin test showed that all the compounds had better acrosin inhibitory activity than that of the control compound TLCK.Among them compound 8a was the most potent one, with IC50 0.098 9 mmol/L. |
| keywords:acrosin inhibitor design synthesis acrosin inhibitory activity benzimidazole |
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