含3-羥基-4H-吡喃-4-酮與3-羥基-1H-吡啶-4-酮新型抗糖尿病藥物之設計與合成

Design and Synthesis of Novel Antidiabetic Agents containing 3-Hydroxy-4H-pyran-4-one and 3-Hydroxy-1H-pyridin-4-one Derivatives

廖子黎(Tzu-Li Liuo)

指導教授 ： 曾誠齊

高雄醫學大學/生命科學院/醫藥暨應用化學研究所/碩士(2005年)

摘要

糖尿病乃當今常見的代謝疾病之一，隨著人們生活品質的提昇及飲食文化的改變，其糖尿病的罹患率有日益增加的趨勢。為了有助於糖尿病的治療及改善糖尿病患者的生活品質，研發治療糖尿病的藥物乃是目前醫學研究的一大方向。
3-羥基-4氫-吡喃-4-酮(3-Hydroxy-4H-pyran-4-one)與3-羥基-4氫-吡啶-4-酮(3-Hydroxy-4H-pyridin-4-one）這類架構的衍生物具有非常廣泛的生物活性，如對鐵的螯合能力、抗氧化能力、殺菌能力、抗癌活性與對抗帕金森氏症等能力。而天然物kojic acid
(1,5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one)能螯合銅而具有抑制酪胺酸酶活性的能力。因此為探求這類結構與活性之間的關連性，我們將此架構接上兩個碳原子及一個芳香雜環，做成類似胰島素增敏劑的結構，並且探討這類化合物的活性，我們期望此類衍生物可成為新型抗糖尿病的製劑。

關鍵字

抗糖尿病藥物

並列摘要

Diabetes mellitus (DM) is one of the metabolic disorders
due to the deficiency of insulin secretion and/or a reduction in the effectiveness of insulin. In order to have more drugs for handling of DM, the present study performed the development of active compounds from natural plants.
3-Hydroxy-4H-pyran-4-one and 3-hydroxy-4H-pyridin-4-one this kind of overhead construction derivatives have exhibited a widespread biological activity, such as the ion-chelative ability, anti-oxidative, anti- bacterial, anti-proliferative and anti-parkinson activities. Kojic acid(1,5-hydroxy-2-(hydroxymethyl)-4H-pyran-4-one) can chelate- copper to suppress tyrosinase activity. In order to explore it’s structure- activity relationships, We have attached two carbon atoms and an aromatic heterocyclic ring to kojic acid, the structure of these compounds similar to insulin sensitizer agents and evaluated then antidiabetic activities. We Expected that this kind of derivatives may become new antidiabetic agents.

並列關鍵字

Antidiabetic Agents

參考文獻

參考文獻

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