羥丙基 -beta- 環糊精與 Quinolines 化合物結構與活性關係之研究

1. 羥丙基-beta-環糊精與Quinolines化合物結構與活性關係之研究羥丙基-beta-環糊精與Quinolines化合物結構與活性關係之研究 • 環糊精於過去數年在各領域有大量的研究，例如，醫藥、化妝品、分析、合成及分子生物等。本實驗主要著眼於環糊精衍生物hydroxypropyl-beta-cyclodextrin與Quinoline類一系列衍生物包覆錯合後所得到的溶解度提升曲線斜率，結果發現Quinoline類化合物的phase-solubility圖大多符合Higuchi 及Connors所提出溶解度型態分類的AL type，也就是quinoline衍生物與HPCD是以1：1化學當量形成包覆錯合物；但是不同的quinoline類衍生物所得到的提升曲線斜率便不同，因此我們以溶解度提升曲線斜率減少率(slope decrement)作為影響的指標。當C4位置接有取代基時，HPCD與之包覆的能力會小於在C2 、C3 或C6位置有取代基者；若是quinoline環上有雙取代基時，溶解度及溶解度提升曲線斜率會小於單取代基；取代基的疏水性(hydrophobicity)會影響化合物溶解度提升的倍數。因此我們可以結論化合物的立體結構、疏水性及取代基所在位置決定HPCD與quinoline類衍生物進行包覆錯合時的程度或難易。

2. Structure Activity Relationship Study of Hydroxypropyl-beta-Cyclodextrin and Substituted Quinolines • The slopes of phase-solubility diagram of HPCD-quinolines complexes were studied in this thesis. It revealed that most of quinoline derivatives fit the AL type of phase-solubility diagram described by Higuchi and Connors with 1：1 molar ratio complex form. If substituted group was at C4 position, the complexing ability of HPCD was lower than substituted group at C2, C3 or C6 position. If there were disubstituted groups, the solubility and slope were smaller than single substituted group. The hydrophobicity of substituted group affact the increment of solubility. We concluded the steric structure of compounds, hydrophobicity and position of substituted group were the main factors affecting the degree of complexation.