源自白桦脂醇的齐墩果烷二羧酸酯类化合物可作为乙酰胆碱酯酶的抑制剂。
Allobetulin derived seco-oleananedicarboxylates act as inhibitors of acetylcholinesterase.
作者信息
Heller Lucie, Schwarz Stefan, Obernauer Anja, Csuk René
机构信息
Martin-Luther-Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
Martin-Luther-Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany.
出版信息
Bioorg Med Chem Lett. 2015 Jul 1;25(13):2654-6. doi: 10.1016/j.bmcl.2015.04.086. Epub 2015 May 5.
Ring opening of allobetulone gave either seco-acid 8 or di-acid 4. These acids were converted into esters that were screened by Ellman's assay. A dibutenylester of low cytotoxicity (NIH 3T3 murine embryonic fibroblasts) was shown to be a good mixed-type inhibitor (Ki=3.39, Ki'=2.26μM) for acetylcholinesterase.
别香橙酮的开环反应生成了裂环酸8或二酸4。这些酸被转化为酯，并通过埃尔曼测定法进行筛选。一种具有低细胞毒性（对NIH 3T3小鼠胚胎成纤维细胞）的二丁烯基酯被证明是乙酰胆碱酯酶的一种良好的混合型抑制剂（Ki = 3.39，Ki' = 2.26μM）。
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