新抗喘药物的研究——茶碱衍生物及卤代苯乙醇胺化合物的合成

本文根据β_2-受体兴奋剂和茶碱类药物的作用机制,结合两类药物的基本结构和构效关系,运用新药设计中的拼合原理及生物电子等排原理,设计扦合成了两类共十六个尚未见于文献报导的化合物。经初步药理实验证明均具有抗哮喘作用,其中I_(5-8)活性较高,且对心脏副作用轻微,可望成为治疗哮喘的新药。     

对－苯二甲酸衍生物的合成及其诱导分化HL－60细胞的活性

作者合成了１３个对－苯二甲酸衍生物，其中有９个化合物尚未见文献报道。通过对ＨＬ－６０细胞诱导分化活性试验，发现有两个化合物在浓度为５×１０￣（－６）ｍｏｌ／Ｌ时，可使细胞分化率达５５％，低于维Ａ酸的分化率（７９％，１０￣（－７）ｍｏｌ／Ｌ）。     

Ionone derivatives from Alternanthera sessilis

The chloroform extract of the air-dried leaves of Alternanthera sessilis afforded a mixture of diastereomers of a new ionone derivative 1 whose structures were elucidated by extensive 1D and 2D NMR spectroscopy and mass spectrometry. Oxidative cleavage of 1 to aldehyde 3 with manganese dioxide confirmed diastereoisomerism arose from a racemic side chain chiral centre. Antimicrobial tests on the mixture of diastereomers and the derivative indicated that they have low activities against Pseudomonas aeruginosa and Trichophyton mentagrophytes.     

卡莫司他衍生物的合成

目的 合成一种具有游离伯胺的卡莫司他衍生物.方法 以对羟基苯乙酸为原料,经4步反应得到目标化合物.结果与结论 成功制备了目标产物,所得产物的化学结构经1HNMR、MS确认.     

医学英语派生词的特点及教学方法探讨

从词源学、构词方法、同义词等几个方面讨论了医学英语派生词的特点，并以此为基础探讨了医学英语派生词的教学方法。     

3,4—二甲氧基苯乙胺类衍生物构效关系研究

用Palygen软件包中的Charmn软件和集团坐标轮换法,对所合成的14个3,4-二甲氧基苯乙胺类衍生物的构象进行计算机模拟。根据所得各化合物的最低能量构象,计算其VDW、偶极距、N原子上的电荷密度等值,并利用化合物的生物活性1gl/IC_(50)(α_1)值,以逐步回归法建立回归方程:y=5.022—0.106X_6—0.0223X_7—0.7975X_8—2.3256X__(12),R=0.8681,F=6.8844>F(0.01)(4.14)。结果提示:方程相关性显著,该系列化合物体现的生物活性与理化参数之间的关系在于苯乙胺衍生物分子的整体作用。     

Investigating the potential of erythromycin and derivatives as chiral selector in capillary electrophoresis

Macrocyclic antibiotics are present in an increasing number of chiral separation applications. In this study, erythromycin and some derivatives, belonging to the group of macrolide antibiotics, were investigated for their potential as chiral selector. Erythromycin A itself and five related substances namely erythromycin A N-oxide, anhydroerythromycin A, anhydroerythromycin A N-oxide, erythralosamine and erythralosamine N-oxide were included. Twenty-one chiral compounds with a wide difference in physico-chemical properties were used to test the chiral activity of the erythromycins. The chiral compounds were analysed using capillary zone electrophoresis with the erythromycins dissolved in the running buffer at different concentrations ranging from 0.1 to 10 mM, with three different BGEs: sodium phosphate pHs 3.0 and 7.0 and sodium borate pH 9.2. The erythromycins showed more interactions with the acidic compounds (as observed with leucovorin, dopa, carbidopa, ketoprofen, indoprofen and warfarin) than with the neutral or weakly basic ones, especially in acidic medium. Unfortunately, no chiral separations were obtained for any of the 21 racemic mixtures. The complexation constants were calculated for the compounds showing interaction, based on the variation of electrophoretic mobility of the compounds in the presence of different concentrations of erythromycins. Finally, the size of erythromycin A was calculated using computational modelling. It was shown that the aglycone ring is only half as big as the β-cyclodextrin cavity, giving a possible explanation for the negative response of erythromycin in this study.     

香草醛葡萄糖苷希夫碱衍生物Ⅳ的合成与结构表征

目的合成一种兼有香草醛活性和希夫碱功效的化合物,筛选具有镇静、抗癫疒间、抗癌的药物。方法用葡萄糖、香草醛为原料,经过乙酰化、溴代等步骤合成了中间体四乙酰葡萄糖香草醛苷,然后与对氯苯胺反应。结果合成了目标化合物Ⅳ。对目标化合物Ⅳ用IR、1HNMR、MS进行结构表征,分析证实所合成的化合物与预期结构一致。结论依据药物拼合原理,可以对香草醛进行结构改造和修饰,合成其希夫碱类化合物。     

鬼臼毒素及其衍生物的波谱特征及药理活性

本文对鬼臼毒素及其衍生物的波谱特征和药理活性进行了系统的综述,为今后的深入研究提供信息和借鉴.     

阿魏酸和咖啡酸衍生物的抗氧化能力研究

采用人血浆低密度脂蛋白（ＬＤＬ）氧化反应体外实验体系，研究了合成的阿魏酸（Ｆｅｒｕｌｉｃａｃｉｄ）和咖啡酸（Ｃａｆｆｅｉｃａｃｉｄ）衍生物的抗氧化性能，并与已知的抗氧化剂ＶｉｔＥ等作了对比。结果显示其中阿魏酸、香草醛肟，及二乙酰基咖啡酸抗氧化能力较强，超过了ＶｉｔＥ，另外五个衍生物抗氧化能力不及ＶｉｔＥ，但均在其功能基因被保护的状态下。本文对抗氧剂的构效关系作了探讨。