奎宁新型聚氮杂环衍生物的合成与生物活性
Synthesis and Biological Activity of Novel Polyazaheterocyclic Derivatives of Quinine.
作者信息
Mukusheva Gulim K, Toigambekova Nurizat N, Seidakhmetova Roza B, Jalmakhanbetova Roza I, Babakhanova Mukhlissa N, Nurkenov Oralgazy A, Akishina Ekaterina A, Dikusar Evgenij A, Kolesnik Irina A, Zhou Hongwei, Potkin Vladimir I
机构信息
Chemistry Faculty, Karaganda Buketov University, Karaganda 100024, Kazakhstan.
Department of Clinical Pharmacology and Evidence-Based Medicine, Karaganda Medical University, Karaganda 100024, Kazakhstan.
出版信息
Molecules. 2025 Aug 7;30(15):3301. doi: 10.3390/molecules30153301.
A synthetic methodology of the CuAAC "click" approach was exploited for the construction of 1,2-azolyltriazole quinine derivatives by the reaction of O-propargylquinine with azidomethyl-1,2-azoles in methanol. Quinine-piperidine and quinine-anabasine conjugates were obtained using a chloroacetate linker by reacting quinine chloroacetate with piperidine or anabasine in a diethyl ether medium. Cinchophene ester was obtained by the acylation of quinine with cinchophen acid chloride in methylene chloride. The antibacterial, fungicidal, analgesic and cytotoxic properties of the obtained compounds were examined.
利用铜催化的叠氮-炔环加成（CuAAC）“点击”方法的合成方法，通过O-炔丙基奎宁与叠氮甲基-1,2-唑在甲醇中反应，构建1,2-唑基三唑奎宁衍生物。通过奎宁氯乙酸酯与哌啶或毒藜碱在乙醚介质中反应，使用氯乙酸酯连接基获得奎宁-哌啶和奎宁-毒藜碱缀合物。通过奎宁与辛可芬酰氯在二氯甲烷中酰化反应得到辛可芬酯。对所得化合物的抗菌、杀菌、镇痛和细胞毒性特性进行了研究。
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