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| 題 名 | Synthesis of Mannich Base Derivatives of Oroxylin A Endowed with Anti-inflammatory Activity=合成具抗發炎活性之木蝶素之曼尼克鹼衍生物 |
|---|---|
| 作 者 | 黃劍銘; 李安榮; 康珮華; 黃文鑫; | 書刊名 | Journal of Medical Sciences |
| 卷 期 | 30:2 2010.04[民99.04] |
| 頁 次 | 頁41-46 |
| 分類號 | 418.2216 |
| 關鍵詞 | 抗發炎; 木蝶素; 曼尼克鹼衍生物; Anti-inflammatory; Mannich base; Oroxylin A; λ-carrageenan-induced rat hind paw edema; |
| 語 文 | 英文(English) |
| 英文摘要 | Synthesis of baicalein, oroxylin A and wogonin, major active constituents of Scutellaria baicalensis GEORGI, was successfully developed in a previous report. In this investigation of novel oroxylin A derivatives as potential anti-infl ammatory agents, a series of Mannich base derivatives at C-8 in A-ring of oroxylin A were designed and synthesized. All the oroxylin A derivatives exhibited signifi cant anti-infl ammatory activity against λ-carrageenan-induced rat hind paw edema (CIPE). The results showed that the target compounds, oroxylin A (4a) and derivatives 4b-i (oroxylin A bearings a 8-substituent as piperidin-1-ylmethyl, morpholin-4-ylmethyl, 4-methyl-piperazin-1-ylmethyl, 4-pyridin-2-yl-piperazin- 1-ylmethyl, 4-pyrimidin-2-yl-piperazin-1-ylmethyl, 4-(2-chloro-phenyl)-piperazin-1-ylmethyl, 4-(4-nitro-phenyl)- piperazin-1-ylmethyl, 4-(4-fluoro-phenyl)-piperazin-1-ylmethyl, respectively) exerted a remarkably anti-inflammatory effect with a signifi cant reduction in swelling. Among them, compounds 4b (8-morpholin-4-ylmethyl oroxylin A), 4c (8-piperidinyl-4-ylmethyl oroxylin A), and 4f (8-[N-(N-2-pyrimidinyl)-piperazin-1-yl]methyl oroxylin A) proved to be the most potent with over 100% inhibition at 20 mg/kg dose in the fi rst hour and potency lasted 5 hours in comparison to that of ibuprofen (as a positive control). |
本系統中英文摘要資訊取自各篇刊載內容。