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本文涉及到以下几个方面的内容：（ⅰ）硫脲类化合物的合成（ⅱ）荧光探针的合成（ⅲ）检测方法的建立及其对可溶性环氧化物水解酶抑制活性的检测。 近年来随着可溶性环氧化物水解酶结构和作用机制的研究，进一步阐明抑制可溶性环氧化物水解酶的活性可治疗多种心血管疾病及炎症。到目前为止，虽然已经研究了好几代抑制剂，但是任存在水溶性、稳定性、选择性等较差的确定；因此继续开发新型可溶性环氧化物水解酶抑制剂已成为研究的热点。本论文在前人工作和查阅大量文献的基础上，设计和合成了一系列硫脲类化合物。 检测化合物的生物活性最常用的方法是：液相、气相、紫外、分光光度计法、荧光法等，但是对化合物进行高通量的筛选时，荧光检测法具有高效、快速、方便且不受其他物质干扰的优点。因此本文借助荧光探针，对可溶性环氧化物酶有抑制活性的硫脲类化合物进行高通量筛选。经后期实验验证了这一方法的可行性，得到了一些具有较好抑制效果的新型化合物。 |
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sltmac(金币+30, 翻译EPI+1): 欢迎常来~~~ 2011-04-17 12:35:26
sltmac(金币+30, 翻译EPI+1): 欢迎常来~~~ 2011-04-17 12:35:26
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This paper involves the following aspects: (Ⅰ) the synthesis of thiourea Derivatives； (Ⅱ) the synthesis of fluorescent probes ； (Ⅲ)the Establishment Of Detection method and Its Detection of soluble epoxide hydrolase activity ； In recent years, with research of the soluble epoxide hydrolase structure and mechanism of action, the soluble epoxide hydrolase activity was further clarified and variety of cardiovascular diseases and inflammationmay be treated. So far, several generations of inhibitors has been studied，but poor water-soluble, poor stability, and poor selectivity were still existed.Therefore， Continue to develop new inhibitors of soluble epoxide hydrolase has become a hot research.On the base of Previous work and access to a large number of literatures. The thesis Designs and synthesizes a series of thiourea compounds. |
2楼2011-04-15 11:19:42
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sltmac(金币+20): 2011-04-17 12:35:32
sltmac(金币+20): 2011-04-17 12:35:32
| Detection of biologically active compounds most commonly used methods are: liquid, gas, UV spectrophotometer, fluorescence methods such as, but high-throughput screening of compounds, the fluorescence detection method is an efficient, fast, easy and free Other substances interfere with the benefits. This article with fluorescent probe, soluble epoxide enzyme inhibitory activity of thiourea compounds for high throughput screening. The latter experiments show the feasibility of this method to obtain good inhibitory effect of some new compounds. |
3楼2011-04-15 11:20:16