5-取代-1H-苯并[d]咪唑-2-基氨基甲酸甲酯衍生物的合成及顶体酶抑制活性。
Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives.
机构信息
Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
出版信息
Bioorg Med Chem Lett. 2012 May 15;22(10):3554-9. doi: 10.1016/j.bmcl.2012.03.042. Epub 2012 Mar 21.
A series of novel methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamates were designed, synthesized, and their acrosin inhibitory activities evaluated in vitro. The results of acrosin inhibitory activity showed that all title compounds were more potent than the control TLCK. Compound 4w displayed the most potent acrosin inhibitory activity among all the compounds, with an IC(50) of 6.3×10(-5)M. The studies provide a new structural class for the development of novel acrosin inhibitory agents.
设计、合成了一系列新型的 1H-苯并[d]咪唑-2-基甲酰胺的 5-取代甲基衍生物，并在体外评价了它们的顶体蛋白酶抑制活性。顶体蛋白酶抑制活性结果表明，所有标题化合物均比对照 TLCK 更有效。在所有化合物中，化合物 4w 显示出最强的顶体蛋白酶抑制活性，IC50 为 6.3×10(-5)M。这些研究为开发新型顶体蛋白酶抑制剂提供了一个新的结构类型。
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