【作者】 冯菊红；

【导师】 刘钊杰； 胡利明；

【作者基本信息】 华中师范大学 ， 有机化学， 2002， 硕士

【摘要】 硒是人体必需的微量元素之一，近三十年来，人们对硒的无机化学，有机化学，生物化学，药物化学，毒性，代谢等方面进行了较为系统的研究，取得了大量的研究成果，发现含硒化合物具有抗菌，抗氧化等活性。本研究采用活性基团拼接原理，设计合成了三个系列32个含硒代吗啉类衍生物，其通式如下： 对含硒化合物的研究进展做了综述，并对课题所涉及到的咪唑啉酮类化合物的研究进展做了介绍。 讨论了中间体硒代吗啉和产物Ⅲ的合成条件。 所合成的新化合物结构均经1H NMR，MS，IR等证实，分析了每个系列化合物的波谱性质。 对所合成的化合物进行了生物活性的测试，结果表明这些化合物均未显示出明显的植物生长调节活性，但表现出抑菌活性。用含毒介质法对所有的化合物进行了杀菌活性测试：化合物Ⅰ、Ⅱ在500ppm对水稻纹枯菌和苹果轮纹菌表现出80％以上的抑制活性；化合物Ⅲ在50ppm对苹果轮纹菌的抑制率达到70％。用微热量法对第一、二系列化合物进行抗菌活性测试，发现第一系列化合物的抗菌活性优于第二系列化合物。其中化合物Ⅱf的活性最好，它的半抑制浓度只有85ng／mL。更多还原

【Abstract】 Selenium is an essential trace element for animal and human health. A great progress has been made in the inorganic chemistry, organic chemistry, biochemistry, pharmaceutical chemistry, toxicity and metabolism of selenium for the last thirty years. This thesis reviews the recent studies about the synthesis and properties of organoselenocompounds.In order to search for new type bioactive organoselenocompounds, based on the principles of the connections of bioactive groups, we designed and synthesized three series derivatives of selenomorpholine,. The formulae of the target compounds were illustrated as follows:Convenient synthetic methods of selemorpholine and imidazolidinone were investigated.The structures of all new compounds were characterized by !H NMR, MS and ER spectroscopes.Preliminary bioassay showed that some of them have fungicidal and antibacterial activity. Fungicidal activity of thirty compounds that contain selenomorpholine was studied by measuring the diameter of fungi growth. The result indicated thirteen compounds reach to the grade of B and can be further investigated as lead compounds.The action of eleven derivatives of selenomorpholine to Escherichia. coli was studied by microcalorimetry. The rate constant k and the half-inhibitory concentration ICso were calculated. II f is the strongest antibacterial compound.Its ICso was 85 g/mL.All compounds didn’t show plant growth regulator activity.更多还原