期刊論文
| 學年 | 99 |
|---|---|
| 學期 | 2 |
| 出版（發表）日期 | 2011-02-01 |
| 作品名稱 | Synthesis of polyhydroxy 7- and N-alkyl-azepanes as potent glycosidase inhibitors |
| 作品名稱（其他語言） | |
| 著者 | Shih, Tzenge-lien; Liang, Ming-tsung; Wu, Kuen-da; Lin, Chun-hung |
| 單位 | 淡江大學化學學系 |
| 出版者 | Oxford: Pergamon |
| 著錄名稱、卷期、頁數 | Carbohydrate Research 346(2), pp.183-190 |
| 摘要 | An effective synthetic method for polyhydroxylated azepanes that contain an alkyl group (Me or Bu) at either the 7- or N-positions is developed. The synthetic routes are accomplished in eight to ten steps from d-(−)-quinic acid. Among the compounds synthesized, the polyhydroxy 7-butyl azepane (compound 3), which possessed the R-configuration at C-7 position, is shown to give potent inhibition against β-galactosidase (IC50 = 3 μM). Preliminary biological data indicate that the length of alkyl groups along with the proper stereochemistry at the C-7 position is essential for acquiring extra binding affinity. Using similar synthetic routes, the polyhydroxy N-methyl and N-butyl azepanes are synthesized for the comparison of their biological activities. |
| 關鍵字 | Azepane; d-(−)-Quinic acid; β-Galactosidase; Glycosidase inhibitor |
| 語言 | en |
| ISSN | 0008-6215 |
| 期刊性質 | 國外 |
| 收錄於 | EI SCI |
| 產學合作 | |
| 通訊作者 | Shih, Tzenge-lien; Lin, Chun-hung |
| 審稿制度 | |
| 國別 | GBR |
| 公開徵稿 | |
| 出版型式 | 紙本 |
| 相關連結 |
機構典藏連結 ( http://tkuir.lib.tku.edu.tw:8080/dspace/handle/987654321/61753 ) |