化学研究
化學研究
화학연구
CHEMICAL RESEARCHES
2014年
5期
449-452
,共4页
田智勇%黄凯%姬卞生%赵瑾%王超杰
田智勇%黃凱%姬卞生%趙瑾%王超傑
전지용%황개%희변생%조근%왕초걸
双喹啉%多胺缀合物%合成%生物活性%测定
雙喹啉%多胺綴閤物%閤成%生物活性%測定
쌍규람%다알철합물%합성%생물활성%측정
bis-quinoline%polyamine conjugates%synthesis%biological activity%determination
为了获得具有高活性的神经元保护药物,以1,3-丙二胺、1,4-丁二胺、1,6-己二胺等为原料,合成了4个新的双喹啉-多胺缀合物;利用核磁共振谱、质谱和元素分析确认了目标化合物的结构,同时评价了它们对神经元细胞的保护作用。结果表明,4个目标化合物对神经元细胞的保护作用均较差,说明多胺链并不能增强喹啉对神经元细胞的保护作用。
為瞭穫得具有高活性的神經元保護藥物,以1,3-丙二胺、1,4-丁二胺、1,6-己二胺等為原料,閤成瞭4箇新的雙喹啉-多胺綴閤物;利用覈磁共振譜、質譜和元素分析確認瞭目標化閤物的結構,同時評價瞭它們對神經元細胞的保護作用。結果錶明,4箇目標化閤物對神經元細胞的保護作用均較差,說明多胺鏈併不能增彊喹啉對神經元細胞的保護作用。
위료획득구유고활성적신경원보호약물,이1,3-병이알、1,4-정이알、1,6-기이알등위원료,합성료4개신적쌍규람-다알철합물;이용핵자공진보、질보화원소분석학인료목표화합물적결구,동시평개료타문대신경원세포적보호작용。결과표명,4개목표화합물대신경원세포적보호작용균교차,설명다알련병불능증강규람대신경원세포적보호작용。
Four novel bis-quinoline-polyamine conjugates were synthesized with 1,3-propanedia-mine,1,4-bytanediamine and 1,6-hexanediamine as the starting materials in order to search drugs with high activity for neuroprotection.The structure of the as-synthesized products were confirmed by nuclear magnetic resonance spectrometry and mass spectrometry as well as ele-mental analysis,and their protection capabitities for neuron cell were evaluated.The prelimina-ry in vitro physiological activities against PC12 cell lines were also assessed.Results show that all the four as-synthesized target products exhibit poor protection capability for neuron cell, which indicates that the presence of the polyamine motif does not contribute to enhancing the protection capability of quinoline for neuron cell.