棉酚与三氮唑类衍生物的合成及抗菌活性研究

Triazole and gossypol's derivatives synthesis and research on antibacterial activity

目的:探讨棉酚与三氮唑类衍生物合成工艺的条件及合成物的抗菌活性,反应条件涉及温度、物料比、反应时间及反应溶剂。方法:通过正交设计寻找最佳工艺,运用熔点测定仪、红外、紫外、核磁共振等检测是否有新物质生成及化学结构,通过TLC监测反应进行程度,用抑菌实验对衍生物的抗菌活性进行研究。结果:棉酚与三氮唑类衍生物合成的最佳工艺的反应温度70℃,反应时间3 h,反应溶剂为无水乙醇,物料比为1:3。结论:生成的衍生物有较强的脂溶性,在优化工艺下进行反应产量较高,为棉酚与三氮唑类衍生物合成提供了较好的方法。

Objective：To study the technologic condition of triazole and gossypol＇s derivatives synthesis,compound＇s antibacterial activity,reaction conditions,involving reaction temperature,ratio of reactants,reaction time and sort of solvent.Methods：The orthogonal experimental design was used to search for the best process,and the melting point apparatus,UV,IR,NMR were adopted to determine whether the new material to be generated and its chemical structure.The extent of reactions was monitored by TLC.The derivatives＇s antibacterial activity was researched by bacteriostatic experiment.Results：The best technologic condition of triazole and gossypol＇s derivatives synthesis was the reaction temperature 70 ℃,the reaction time 3 h,anhydrous ethanol as solvent and the ratio of reactants was 1：3.Antibacterial experiment had no obvious effect.Conclusion：The generated derivatives have strong fat-solubility.Under the optimized technologic condition,the reaction has high yield,which provides a good method to synthesize triazole and gossypol＇s derivatives.