本文選題：硫色滿酮 + 一鍋法��； 參考：《河北大學(xué)》2014年碩士論文

【摘要】：硫色滿酮類化合物是一類高脂溶低水溶性的含硫雜環(huán)化合物，具有廣泛的生理藥理活性，它通過對真菌細胞壁和細胞膜結(jié)構(gòu)和功能的破壞，達到抑制真菌生長的目的。 本文基于對硫色滿酮的修飾設(shè)計并一鍋法合成了19個苯基噻唑-硫色烯并[4,3-c]吡唑類化合物和15個吡喃并[3,2-c]噻喃類化合物。所得到的目標化合物結(jié)構(gòu)由核磁共振氫譜及碳譜、高分辨質(zhì)譜等確證。并采用二倍濃度稀釋法對目標化合物的抗真菌活性進行了測試。 苯基噻唑-硫色烯并[4,3-c]吡唑類化合物以取代苯硫酚為起始原料，合成中間產(chǎn)物3-醛基硫色滿酮，再以3-醛基硫色滿酮，，溴代苯乙酮和氨基硫脲為原料一鍋法得到19個目標產(chǎn)物。體外抗真菌實驗表明部分化合物對新生隱球菌有較好的抑制活性。對比了不同溶劑和反應(yīng)時間條件下回流法和超聲法對該反應(yīng)產(chǎn)率的影響，結(jié)果表明在超聲條件下以乙醇為溶劑反應(yīng)產(chǎn)物的產(chǎn)率最高。 吡喃并[3,2-c]噻喃類化合物以取代苯硫酚為原料，合成中間產(chǎn)物取代硫色滿酮。再以取代硫色滿酮，丙二腈和芳醛為原料一鍋法得到15個目標產(chǎn)物。部分化合物對新生隱球菌有微弱的抑制作用。
[Abstract]:Sulfur and ketones are a kind of heterocyclic compounds with high lipid solubility and low water solubility. They have a wide range of physiological and pharmacological activities. It can inhibit the growth of fungi by destroying the cell wall and cell membrane structure and function. In this paper, 19 phenythiazole-thioleno [4o _ 3-c] pyrazole compounds and 15 pyrano [3o _ 2-c] thiopyranes were synthesized by one-pot method based on the modification design of p-thiolone. The structure of the target compounds was confirmed by nuclear magnetic resonance spectroscopy (NMR), carbon spectrum, high resolution mass spectrometry and so on. The antifungal activity of the target compound was tested by double concentration dilution method. Phenylthiazole-thiocereno [4o 3-c] pyrazole was synthesized from substituted phenythiophenol as starting material, and then 19 target products were obtained by one-pot method using 3-aldothiolone, bromoacetophenone and thiosemicarbazone as raw materials. Antifungal experiments in vitro showed that some compounds had good inhibitory activity against Cryptococcus neoformans. The effects of reflux method and ultrasonic method on the yield of the reaction were compared under different solvent and reaction time. The results showed that ethanol was the best solvent under ultrasonic conditions. In this paper, the intermediate product of substituted thiolone was synthesized from substituted phenythiophenol by pyrano [3o 2-c] thiofuran compounds. Fifteen target products were obtained by one-pot method using substituted thiolone, malonitrile and aromatic aldehydes as raw materials. Some compounds have weak inhibitory effect on Cryptococcus neoformans.
【學(xué)位授予單位】：河北大學(xué)
【學(xué)位級別】：碩士
【學(xué)位授予年份】：2014
【分類號】：R914

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