【作者】 李世学；

【导师】 刘建利；

【作者基本信息】 西北大学 ， 中药学， 2009， 硕士

【摘要】 含有茚二酮骨架的化合物具有良好的生物活性,茚并吡啶类化合物和茚并喹啉类化合物在医药学、农药学等领域的应用日见报道。研究成果涉及抗癌、抗炎/抗过敏、抗心血管硬化、杀菌、除草等方面。为了拓展茚酮类化合物的合成和应用研究,本文合成了系列茚酮类化合物,并对合成化合物进行了抑菌活性研究,获得了具有理论和实际意义的研究结果。第二章共合成4个1,3-茚二酮化合物,通过条件实验选择,优化了反应条件,利用红外光谱、核磁共振氢谱对产物进行了表征。第三章合成了13个2-苯亚甲基-1,3-茚二酮和10个2-苯亚甲基-4-硝基-1,3-茚二酮化合物,经红外光谱和核磁共振氢谱对合成化合物进行了表征,其中有10个化合物未见文献报道。第四章合成了7个3-氨基苯-1H-1-茚酮化合物,经红外光谱、核磁共振氢谱对对这些化合物进行了结构表征,其中4个化合物未见文献报道。第五章合成了4个茚并吡啶类化合物,经红外光谱、核磁共振氢谱对合成化合物进行了结构表征,其中3个未见文献报道。第六章对合成化合物的抑菌活性进行了研究。从实验结果来看,大部分2-苯亚甲基-4-硝基-1,3-茚二酮类化合物抑菌活性较好;7个3-氨基苯-1H-1-茚酮化合物中有3个具有抑菌活性,其中两个的抑菌活性较强,值得进一步研究。第七章初步讨论了茚酮类化合物的构效关系。更多还原

【Abstract】 A large number of compounds containing indanone skeleton showed good biological activity, such as anti-cancer, anti-inflammatory / anti-allergic, anti-cardiovascular sclerosis, bactericidal, weeding and so on. Indenopyridines and indenoquinolines were used in medicine and pesticide widely. In order to further enlarge the application of indanone derivatives, we design and synthesize some indanone derivatives and evaluate their antimicrobial activities.In the ChapterⅡ, four 1, 3-indandiones have been synthesized. The best reaction conditions have been optimized by a series of tests. The structures of the synthetic compounds were confirmed by ~1H-NMR and IR spectra. In the ChapterⅢ, thirteen 2-arylidene-l, 3-indandiones and ten 2-arylidene-4-nitro- 1, 3- indandiones have been synthesized, of which ten are new compounds. The structures of the synthetic compounds were confirmed by ~1H-NMR and IR spectra. In the ChapterⅣ, seven 3-phenylamino-1H-inden-1-one compounds have been synthesized, of which four are new compounds. The structures of the synthetic compounds were confirmed by ~1H-NMR and IR spectra. In the ChapterⅤ, four indenodihydropyridines have been synthesized, of which three are new compounds. The structures of the synthetic compounds were confirmed by ~1H-NMR and IR spectra. In the ChapterⅥ, the antibacterial activities of the synthetic compounds were studied. Most of 2-arylidene-4-nitro- 1, 3- indandiones compounds showed a certain degree of antibacterial activity. 2-arylidene-4-nitro- 1, 3- indandiones is a potential antibacterial agent. Three 3-phenylamino-1H-inden-l-one derivatives showed antibacterial activity, two of which have the strong antibacterial activity. It is worth further study. In the ChapterⅦ, a preliminary structure- activity relationship of indene derivatives was discussed.更多还原