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- Synthesis and Pharmacological Effects of Tetramethylpyrazine Derivatives
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題名 | Synthesis and Pharmacological Effects of Tetramethylpyrazine Derivatives=四甲基吡衍生物之合成及藥理活性 |
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作者 | 李安榮; | 書刊名 | 醫學研究 |
卷期 | 13:1 1992.07[民81.07] |
頁次 | 頁41-50 |
分類號 | 414.5 |
關鍵詞 | 四甲基吡; 合成; 活性; 衍生物; 藥理; |
語文 | 英文(English) |
中文摘要 | 四甲基吡□(1)為中藥川芎之有效成分。川芎自古即用於解除頭、胃疼痛及治療心血管疾病。文獻報導四甲基吡□在實驗動物具有良好之增加冠狀循環血流,抑制血管平滑肌收縮,及減低血氧過少之作用。本品已在國外進行臨床試驗,並証明對冠狀循環疾病之療效,但四甲基吡□之缺點為水溶性不佳,且治療劑量較大。 本實驗設計並合成出一系列四甲吡□基衍生物。藉由質子化、氧化及引入親水基團,製備多種產物,以改善水溶性及增進藥理活性。本研究計獲得合成產物八個,其中2,3-二氫吡□(4a)顯示極強之藥理活性及良好水溶性。 |
英文摘要 | The preparation, physicochemical properties and pharmacological effects on the cardiovascular system of 8 tetramethylpyrazine (TMP) derivatives are described. Protonation, oxidation, and incorporation of hydrophilic radicals were employed in the chemical modifications, in an attempt to improve the aqueous solubility and the potency of cardiovascular activity of TMP. Of the compounds synthesized, 2,3-Dihydropyrazine (4a) showed most potent in the relaxant effect on dog coronary and basilar artery and induced early after-depolarization in ventricular tissues. |
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