哌啶并[2,3-b]哌嗪类衍生物的设计、合成及其抗血小板聚集活性研究

以2,3-二氨基吡啶和2,3-丁二酮为起始原料,经环化、催化氢化和亲核取代反应合成了10个新型哌啶并[2,3-b]哌嗪类衍生物(3a~3j),其结构经¹H NMR、¹³C NMR和HR-MS确证。体外抗血小板聚集活性研究表明,化合物3d、3e、3g、3h和3j具有一定的抗血小板聚集作用,其中化合物3h(IC₅₀=1.24mmol/L)的活性显著优于母体化合物川芎嗪(IC₅₀=3.96mmol/L)和阳性药物阿司匹林(IC₅₀=2.41mmol/L)。     

山东鲁抗立科药业有限公司(原山东鲁抗医药股份有限公司树脂分厂)

正山东鲁抗立科药物化学有限公司是山东鲁抗医药股份有限公司与上海立科药物化学有限公司的合资公司,新公司继续持有"鲁抗树脂"的品牌并继续研发和生产药用功能树脂。按照国家食品药品监督管理局[2000]56号文件要求,我们就药用级树脂做了大量工作,就树脂的物理性参数、有机残留控制、动物毒性试验请权威部门做了公正的检测。同时,我公司经过GMP、ISO9001、ISO14001认证,具备生产药用树脂的能力。     

N-Fluorinated phenyl-N＇-pyrimidyl urea derivatives： Synthesis,biological evaluation and 3D-QSAR study

With the increase of herbicide-resistant weeds, novel, more selective and even more potent herbicides to control weeds are needed. In this paper, a series of N-fluorinated phenyl-N＇-pyrimidyl urea derivatives were synthesized and screened for their herbicidal activities against Amaranthus retroflexus （AR） and Setaria viridis （ SV）. Compound 2S （N-（3-trifluoromethylphenyl）-N＇-（2-amino-4-chloro-6-methylpyr- imidyl） urea） exhibited marked herbicidal activity against SV（IC50 =11.67 mg/L） and is more potent than bensulfuron （IC50= 27.45 mg/L）, a commercially available herbicide. A statistically significant CoMFA model with high prediction abilities （q2 = 0.869, r2 = 0.989） was obtained.     

科学家模仿天然珍珠质结构制造新型陶瓷材料

<正>《自然-材料学》报道一种制造简便、强度硬度高的陶瓷材料,这种陶瓷材料可模拟天然珍珠质(包在珍珠外层的一种坚硬物质)的实体结构。这种陶瓷材料在600℃高温时仍可保持其性质,可应用于能源相关和运输安全相关的结构材料。陶瓷属于易碎物质。为了增强韧性,可在其成分中添加变形后不会发生断裂的聚合物和金属。但     

具有抗生物污染活性的分子筛膜用于高效油水分离

The development of the global economy has been accompanied by frequent oil spills caused by accidental leaks and industrial manufacturing, which have seriously threatened the aquatic environment and human health. Traditional methods for the treatment of oily wastewater include centrifugation, skimming, flotation, oil-absorbing technology, etc., which are limited by low separation efficiency as well as secondary pollution during the post-processing of oil absorption materials. Recently, separation technologies utilizing the special wettabilities of filtration membranes have been developed to enrich and recycle oils from wastewater. Among these, the fabrication of superhydrophilic/underwater superhydrophobic membranes have attracted intensive research interest, which can selectively allow the passage of water through the membrane while blocking the oils. However, microorganisms are more likely to breed on these hydrophilic surfaces, eventually leading to the blockage of the membranes. In this study, ZSM-5 zeolite crystals (MFI topological structure) were coated onto the stainless-steel meshes by means of seeding and secondary hydrothermal growth. Then, 70% of the total Na⁺ ions in the zeolite channels were substituted by Ag⁺ ions via an ion exchange process. The resultant membranes (Ag@ZCMFs) were superamphiphilic in air, with both water contact angle and oil contact angle of approximately 0°. However, they became superoleophobic when immersed in water, and the underwater oil contact angle reached 151.27° ± 4.34°. In terms of special wettability, Ag@ZCMF achieved efficient separation for various oil-water mixtures with separation efficiencies above 99%. The water flux and intrusion pressure of Ag@ZCMF depended on the diameter of pinholes in the membrane, which could be modulated by altering the time of secondary hydrothermal growth. For instance, the average diameter of pinholes in Ag@ZCMF with optimum secondary growth time of 14 h (Ag@ZCMF-14) reached approximately 21 μm, giving rise to the water flux and intrusion pressure of 54720 L·m^-2·h^-1 and 4357 Pa, respectively. The anti-corrosion test and rubbing test confirmed the high chemical and mechanical stability of Ag@ZCMF-14, respectively. The separation efficiency of Ag@ZCMF-14 remained stable during ten purification-regeneration cycles, and no obvious attenuation was observed, proving the high separation stability of Ag@ZCMF-14. Furthermore, the loaded Ag⁺ ions afforded the membrane excellent anti-biofouling activity, which could effectively inhibit the growth of both alga and bacteria in the operating environment, thus preventing membrane blockage during the oil-water separation process. In particular, the bacteriostatic rate of Ag@ZCMF-14 to Escherichia coli reached to 99.6%. These results demonstrate that Ag@ZCMFs with anti-biofouling activity has promising potential future applications in the removal of oil slicks from oily wastewater.     

聚(2-甲基-2-噁唑啉)在毛细管电泳分离蛋白质中的应用

毛细管电泳作为一种常见的液相分离技术,因其分析速度快、分离效率高、样品消耗量少等特点,在蛋白质分离分析领域有广泛应用。然而,常用的熔融硅毛细管容易吸附蛋白质,导致电渗流不稳定,分离结果重现性变差;此外,商用毛细管电泳中常用的紫外检测器由于光程短,使得毛细管电泳的检测灵敏度往往不能达到低丰度蛋白质的直接分析要求。因此寻找能够阻止蛋白质吸附、同时能够提高检测灵敏度的涂层是毛细管电泳分离分析蛋白质的重要课题之一。聚（2-甲基-2-噁唑啉）（PMOXA）作为一种类肽类亲水性聚合物,具有与抗蛋白质吸附聚合物聚乙二醇类似的亲水性、抗蛋白质吸附性和生物相容性,而且其类肽结构使之具有较聚乙二醇更好的稳定性,因此近年来在生物质传递、药物载体和阻抗蛋白质吸附等领域得到越来越多的应用。该文主要从两个方面对聚（2-甲基-2-噁唑啉）在毛细管电泳中的应用进行了阐述。一是利用多巴胺作为黏合层将其涂覆在毛细管内壁作为抗蛋白质吸附涂层,这种涂层不仅能成功分离多种蛋白质的混合物（如溶菌酶、细胞色素C、核糖核酸酶A和α-胰凝乳蛋白酶原A）,而且在定量检测奶粉中三聚氰胺、乳铁蛋白的过程中,能阻抗其他蛋白质的非特异性吸附,提高了毛细管电泳对奶粉中三聚氰胺、乳铁蛋白的检测效率。二是将其与具有刺激响应性的聚合物（如聚丙烯酸）构成二元混合刷涂层,在一定的pH和离子强度条件下,涂层可吸附目标蛋白质（如牛血清白蛋白、溶菌酶）,在另一pH和离子强度条件下可将吸附的目标蛋白质全部释放,同时在释放过程中,处于涂层表面的聚（2-甲基-2-噁唑啉）会进一步阻止蛋白质的吸附,释放的蛋白质在电渗流和电泳的双重作用下快速迁移,到达检测器的蛋白质瞬时浓度大大增加,使目标蛋白质得到富集,目标蛋白质的检测信号得到放大,从而达到了提高低丰度蛋白质检测灵敏度的目的。此外,该文还对聚（2-甲基-2-噁唑啉）在毛细管电泳分离蛋白质中的未来发展趋势进行了展望。     

富马酸丙酚替诺福韦合成工艺改进

对富马酸丙酚替诺福韦的合成工艺进行了改进,以干燥的替诺福韦为起始原料,与亚磷酸三苯酯反应得到(R)-9-(2-(苯基磷酰基甲氧基)丙基)腺嘌呤（3）; 3被氯化亚砜氯代得(R)-9-(2-(((苯基)(氯代)(磷酰基)甲氧基)丙基)腺嘌呤（4）; 4与L-丙氨酸异丙酯盐酸盐缩合得9-((R)-2-(((S)-((1-(异丙氧基羰基)乙基)氨基)苯氧基磷酰基)甲氧基)丙基)腺嘌呤（5）; 5经析晶纯化得9-((R)-2-(((S)-（((S)-1-(异丙氧基羰基)乙基)氨基)苯氧基磷酰基)甲氧基)丙基)腺嘌呤（丙酚替诺福韦,6）; 6与富马酸成盐得富马酸丙酚替诺福韦,其结构经¹H NMR, ¹³C NMR, MS(ESI),元素分析和XRD确证。按改进工艺进行公斤级规模放大,产品总收率达到32.2%,化学纯度99.92%,非对映异构体纯度99.99%。     

火灾与撞击联合作用下钢管混凝土柱力学性能研究

为研究火灾高温与撞击联合作用下钢管混凝土柱的力学性能,基于ABAQUS建立了高温作用下考虑轴力影响的钢管混凝土柱侧向撞击有限元模型。首先,对高温与撞击联合作用下考虑轴力影响的钢管混凝土柱的破坏模式与受力全过程进行了分析,探讨了高温下钢管混凝土柱的抗撞性能与工作机理;其次,重点研究了受火时间、材料强度、含钢率以及撞击能量对抗撞性能的影响,并给出了相关设计建议。研究结果表明:高温与撞击联合作用下,钢管混凝土柱主要发生受弯破坏;受火15 min后,构件抗撞性能明显降低。轴压力对构件抗撞性能产生不利影响,轴压比从0增加到0.2,受火60 min构件抗撞性能下降了7.8%;混凝土强度对高温下钢管混凝土柱抗撞性能有显著影响,受火90 min后,混凝土强度由30 MPa增加到50 MPa,构件抗撞性能提高约85%;外钢管强度与含钢率对高温下抗撞性能影响不大。     

不同直径碳纳米管的抗电化学氧化性

本文比较了由化学气相沉积法制备的不同直径(在100 nm以内)的多壁碳纳米管(CNT)的抗电化学氧化性.将CNT电极于1.2 V(vs.RHE)下电氧化120 h,记录氧化电流~时间变化曲线;X射线光电子能谱(XPS)分析氧化前后CNT的表面化学组成.结果表明,随着CNT直径的减小,其氧化电流降低,但其中以为10~20 nm的CNT电极氧化电流最小,表面氧的增量也最小,即被氧化的程度最低,抗电化学氧化性最强.根据不同直径CNT的缺陷位、不定型碳的丰度和碳原子的应力能,分析了其抗电化学氧化性差异的原因.     

姜黄素类似物的合成及其清除自由基的研究

姜黄素(见图1)为中药姜黄的主要成分,是一种黄色色素。研究报道姜黄素具有抗氧化、抗炎、抗病毒、抗癌等生物活性[1-4]。本文通过芳香醛和环己酮催化缩合反应合成了一系列姜黄素类似物(见图2),研究了它们抗自由基的活性。图1姜黄素的化学结构F ig.1 Chem ical structure of cur