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研究生:鄭豐盛
研究生(外文):Feng-Sheng Cheng
論文名稱:氟喹諾酮化合物之合成與抗結核桿菌活性評估
論文名稱(外文):Synthesis and Antibacterial Evaluation of Fluoroquinones Against M.Tuberculosis
指導教授:陳義龍
指導教授(外文):Yeh-Long Chen
學位類別:碩士
校院名稱:高雄醫學大學
系所名稱:藥學研究所碩士在職專班
學門:醫藥衛生學門
學類:藥學學類
論文種類:學術論文
論文出版年:2005
畢業學年度:93
語文別:中文
論文頁數:49
中文關鍵詞:氟喹諾酮
外文關鍵詞:Fluoroquinones
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氟喹諾酮類抗菌藥物中數種作為治療結核桿菌(Mycobacterium tuberculosis)感染的藥物具有很好的化學療效,因為這類藥物對細胞具良好穿透性且經由口服能迅速吸收。在這些特性當中,新抗結核桿菌劑設計的主要原因為傳送化合物通過結核菌之細胞壁,因為結核桿菌細胞表面為具有脂質之有機體組成而形成一道傳送障壁。
因此我們研究的方向,先合成N-1苯基取代的氟喹諾酮增加其親脂性,接著在碳-7位置以肼(hydrazine)取代形成腙類化合物,並在其氮上以各種雜環醛類取代,我們期望結合氟喹諾酮與抗結核桿菌藥物如INH來改進臨床上抗結核桿菌的吸收力及穿透率,因為這些氟喹諾酮衍生物由兩個抗結核桿菌活性基組成而有不同的作用機轉,而希望有更好的藥效。
Some of the fluoroquinolone drugs have been examined as potential chemotherapeutics for Mycobacterium tuberculosis infection; They have the characters of well cell penetration and easy absorbed after oral administration. Therefore, one of the major factor relevant to the design of new antituberculosis agent is the transportation of compounds through the cell wall of mycobacteria. It is well-know that mycolic acids and surface associated lipids of these organisms form a transport barrier which prevent compounds from passing through the cell wall of mycobacteria.
The aims of this study include: (1) synthesize N1-phenyl substituted quinolone to improved lipophilicity; (2) synthesize 7-hydrazinyl substituted N1-arylquinolone with different heterocyclic substituents at the hydrazine. We expected that with the presence of both fluoroquinolone and hydrazone will improve the absorption and cell penetration of these clinically antituberculosis drugs. Fluoroquinolone derivatives consist of two active antituberculosis drugs with different action mechanis, We expect these compounds to be more potent than simply the drug combination.
中文摘要 --------------------------------------------------- p.2
英文摘要 --------------------------------------------------- p.3
壹、緒言 --------------------------------------------------- p.4 -10
一、前言 ---------------------------------------------- p.4
二、研究動機 ---------------------------------------- p.5
貳、合成方法 --------------------------------------------- p.11 - 13
參、藥理活性測試實驗方法與活性結果討論 ------ p.14 - 15
一、實驗方式 ---------------------------------------- p.14
二、活性結果與討論 ------------------------------- p.15
肆、實驗部份 --------------------------------------------- p.16 - 46
一、溶劑及處理過程 ------------------------------- p.16
二、儀器及試藥 ------------------------------------- p.18
三、各化合物的製備 ------------------------------- p. 19
伍、參考文獻 --------------------------------------------- p. 47 - 49
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