臺灣博碩士論文加值系統

中文摘要
本論文為N-取代芐基氨茴酸類緣物(benzyl anthranilic acid analogs )結構與活性的關係(structure and activity relationship; SAR)的研究及合成的衍伸，筆者合成了第I-VI類化合物。
第I-VI類的化合物中並以GM1酵素結合免疫附法(GM1-ELISA)評估標的化合物對下痢活性，篩選結果顯示化合物第VI類中的47、48、49對於與忌熱型腸毒素(LTB)競爭GM1接受器的結合有明顯的抑制作用，而化合物49，經一步動物實驗結果試驗表現出明顯的抗下痢作用。
因此，化合物47可以當成是一個新型且具有開發潛能的抗下痢藥物。

Abstract
As part of a continuing search for potential antidiarrhea agent in benzyl anthranilic acid analogs, a series of compounds I-VI were designed synthesized.
Antidiarrheal activity of synthesized compounds were evaluated. Compounds Ethyl 2-(4-acetoxy-3-methoxy benzylamine) benzoate (47) 、Ethyl 2-(4-hydroy-3-methoxy benzylamine) benzoate (48)、2-(4-hydroxy-3-methoxy benzylamine) benzoic acid (49) showed significant inhibitory effect on the binding of (Heat-labile enterotoixn B subunit；LTB ) to GM1 by GM1-ELISA (Enzyme-liked Immunosorbent Assay). Among them, compound 47 exhibited significant antidiarrheal effect on the LT-induced fluid accumulation in ileal loop.
Therfefore, compound 47 was identified as a new protential antidiarrnea agent.

正文目錄
中文摘要
英文摘要
第一章 緒論 第001頁
第一節忌熱性腸毒素的致瀉機轉 第001頁
第二節氨茴酸與水楊酸衍生物的藥理活性 第007頁
第三節配醣體的吸收代謝及其合成方法之研究概況 第009頁
第四節 免疫分析法的原理 第015頁
第二章 研究動機與目的 第016頁
第三章 結果與討論 第024頁
第一節 化學合成 第025頁
壹4-acetoxy-3-methoxy benzyl chlorid 3 第025頁
貳2-Substituted Phenylbenzamide類13-20 第031頁
參2-Substituted Phenylbenzamide類25-28 第036頁
肆 Methyl substituted baenzoate類 35-41 第041頁
伍 2-Substituted benzyloxybenzoic acid類 45-49 第046頁
陸Salicylic acid-Glucosylation類52-56 第050頁
捌 2-[(4-hydroxy-3-methoxy)benzylamino] benzoic acid-
Glucosylation 57 第055頁
第二節 GM1-ELISA的抗下痢活性試驗 第063頁
第三節 腸毒素下痢分析 第070頁
第四節 藥理活性與分子模擬 第071頁
第四章 結論 第074頁
第五章 實驗部份 第079頁
第一節 化學與藥理試驗的試藥、溶媒與材料 第079頁
一、化學試藥 第079頁
二、化學溶媒 第080頁
三、化學材料 第081頁
四、藥理試驗規格與材料 第082頁
第二節 重要儀器 第083頁
第三節 化合物的製備 第085頁
參考文獻 第126頁
附錄(1)圖譜數據 第131頁
附錄(2)實驗代號 第186頁

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