葛根素衍生物及其转化的吡唑类化合物的合成研究化学专业论文.docxVIP

通过实验测试产物在水中的溶解性，结果表明溶解性能良好，基本满足临床 通过实验测试产物在水中的溶解性，结果表明溶解性能良好，基本满足临床 应用的需要。对吡唑类化合物进行了体外抑菌活性测试，其对选用的两种革 兰氏阴性菌和两种革兰氏阳性菌均有良好的抑菌效果，部分产物的最小抑菌 浓度(MIC)接近阳性对照，有望成为一类新的抑菌剂。 关键词：葛根素衍生物，3,4．二苯基吡唑类化合物，合成，抑菌活性 Ⅱ 万方数据 RESEARCH RESEARCH ON THE SYNT咖SIS 0F PUERAmN DERn7：舡IVES AND THE CONVERTED PYRAZOLE CoMPoUNDS ABSTRACT Puerarin is a natural occurring isoflavone extracting from puerarin lobata or puerarin thomsonii，which is mainly used for the treatment of cardio-cerebrovascular diseases in clinical medicine，such as angina，coronary heart disease，myocardial infarction，etc．The water．soluble，oil．soluble and bioavailability of puerarin are relatively low owing to its structure of isoflavone． Puerarin derivatives can be obtained by modifying the structure of puerarin， which not only can keep the original treatment effect，but also improve its solubility．The pyrazole compounds can be obtained using the reaction of hydrazine hydrate and puerarin derivatives．ne 3，4一diarylpyrazole compounds have good biological activity,which show the effect such as good antitumor, bacteriostat and weight loss．At the same time，these compounds have the advantages of high efficiency,low toxicity and can be used as the lead compound in the process of drug development．As glycosyl is a structure that has more hydroxyl which easy to form hydrogen bonds，make the target molecules combine with target more effectively,change its solubility and guidance，and enhance the receptor affinity ability．Due to the instroduction of glycosyl，the biological activity and physiological function of 3,4-diarylpyrazole compounds were enchanced． In this paper,puerarin derivatives and pyrazole compounds were synthesized．1 5 puerarin derivatives were synthesized by the alkylation reaction of phenolic hydroxyl group and electrophilic substitutive reaction of aromatic ring，using puerarin as raw material．1 l of them increase solubility in organin solvent，4 in the water solubility increase．Among these puerarin derivatives， 7-butoxypuerarin