吡啶联噻唑类药物分子的合成及生物活性研究

发布时间：2017-12-28 00:32

本文关键词：吡啶联噻唑类药物分子的合成及生物活性研究　出处：《云南大学》2016年硕士论文　论文类型：学位论文

【摘要】：含氮杂环结构的化合物在当前医药及农药的创制应用中扮演着越来越重要的角色,其中吡啶、噻唑类化合物由于具有广泛的生物活性从而成为新医药及农药研究的重点和热点。本文的主要工作是合成了几种新型的毗啶联噻唑类化合物以及对其生物活性的研究。论文主要从以下面四个方面进行研究探讨。一、从药理和农药方面总结了吡啶类化合物、噻唑类化合物的研究进展。二、以半胱氨酸盐酸盐和氰基取代的吡啶类化合物为原料出发经过关环、取代、缩合等反应合成了34个吡啶联噻唑类酰胺,22个吡啶联噻唑类酯及4个其他吡啶联噻唑类化合物,对其合成条件进行了探讨,并对其反应的条件进行优化。三、研究表明新型吡啶联噻唑类酰胺、吡啶联噻唑类酯及其他吡啶联噻唑类化合物对丁香假单胞菌的生长均具有抑制作用,为新农药的创制积累了数据。四、在DNA TopoⅡ抑制实验中,吡啶联噻唑类酰胺、吡啶联噻唑类酯都表现出明显的抗癌效果。
[Abstract]:Nitrogenous heterocyclic compounds play an increasingly important role in the creation and application of pharmaceuticals and pesticides. Pyridine and thiazole compounds become the focus and hotspot of new medicine and pesticide research because of their wide biological activities. The main work of this paper is to synthesize several new vishidazole compounds and their biological activities. The thesis is mainly discussed in the following four aspects. First, the research progress of pyridine compounds and thiazole compounds is summarized from the aspects of pharmacology and pesticides. Pyridine compounds two, cysteine hydrochloride and cyano substituted as starting materials through cyclization, substitution, condensation reaction of 34 pyridine thiazole amide thiazole pyridine, 22 esters and 4 other pyridine thiazole compounds, the synthesis conditions were studied, and the reaction of the optimization of the conditions. Three, studies have shown that new pyridinium thiazolides, pyridyl thiazolides and other pyridinium thiazole compounds have inhibitory effects on the growth of Pseudomonas Syringa, and accumulate data for the creation of new pesticides. Four. In the DNA Topo II inhibition test, pyridyl thiazole amides and pyridyl thiazolides have obvious anticancer effects.
【学位授予单位】：云南大学
【学位级别】：硕士
【学位授予年份】：2016
【分类号】：O626.25

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