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本文涉及到以下幾個方面的內(nèi)容:(。┝螂孱惢衔锏暮铣桑áⅲ晒馓结樀暮铣桑á#z測方法的建立及其對可溶性環(huán)氧化物水解酶抑制活性的檢測。 近年來隨著可溶性環(huán)氧化物水解酶結(jié)構(gòu)和作用機(jī)制的研究,進(jìn)一步闡明抑制可溶性環(huán)氧化物水解酶的活性可治療多種心血管疾病及炎癥。到目前為止,雖然已經(jīng)研究了好幾代抑制劑,但是任存在水溶性、穩(wěn)定性、選擇性等較差的確定;因此繼續(xù)開發(fā)新型可溶性環(huán)氧化物水解酶抑制劑已成為研究的熱點(diǎn)。本論文在前人工作和查閱大量文獻(xiàn)的基礎(chǔ)上,設(shè)計和合成了一系列硫脲類化合物。 檢測化合物的生物活性最常用的方法是:液相、氣相、紫外、分光光度計法、熒光法等,但是對化合物進(jìn)行高通量的篩選時,熒光檢測法具有高效、快速、方便且不受其他物質(zhì)干擾的優(yōu)點(diǎn)。因此本文借助熒光探針,對可溶性環(huán)氧化物酶有抑制活性的硫脲類化合物進(jìn)行高通量篩選。經(jīng)后期實(shí)驗驗證了這一方法的可行性,得到了一些具有較好抑制效果的新型化合物。 |
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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. |
| 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. |
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