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Study On The Phosphated Structure Modification And Character Of Puerarin

Posted on:2007-08-25Degree:MasterType:Thesis
Country:ChinaCandidate:J W YuanFull Text:PDF
GTID:2144360185471586Subject:Medicinal chemistry
Abstract/Summary:PDF Full Text Request
Puerarin, which has comprehensive pharmacological action, is maily used clinically for treatment of cardiovascular system diseases, e.g. arrhythmia, cardiac angina, coronary heart disease, myocardial infarction, heart failure, hypertiesia, cerebral edema. The recent studies on pharmacological action, extracting and isolating, pharmaceutics and structural modifications of puerarin were reviewed by this paper.Puerarin is an isoflavone compound. Though it has extensive pharmical values in clinic, there are some flaws to confine its pharmic effects, to some extent, for example, low dissolvality and low imbibition. In order to change its coefficient for n-octanol/water and increase its pharmacological and biologic activity, the research works on this paper conclude the following.1. This paper designed and synthesized eighteen puerarin derivatives, including fifteen novel compounds. The structures of compounds were determined by ESI-MS, NMR and IR. Especially, it was interesting that two sets of signals were observed in the NMR measurements of the compound at the room temperature. By 2D NMR, the data of NMR spectra were assigned completely.2. The compound's conformation of P2 was researched to make use of dynamic NMR and chemical calculation. The result found there were two kinds of different conformer isomers by dynamic NMR. We carried out the conformational analysis using chemical calculation, finally we obtained two preferred conformations and energy values of the compound P2.3. The reaction activity of 7, 4'-OH for the puerarin was researched by the phosphated and ethylized reaction. The result indicated 7-OH of the puerarin was more active than 4'-OH and this difference was decided by the puerarin's structure. The character of NMR spectra was an important proof to judge the reactive place.
Keywords/Search Tags:puerarin, phosphated, Dynamic NMR, conformational research, chemical calculation
PDF Full Text Request
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