Design and synthesis of cyclic acylguanidines as BACE1 inhibitors

Based on the lead compound 1 reported in literature, a series of novel BACE1 inhibitors were designed and synthesized, among which compound 11 exhibited a 14-fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD.     

An amphiphilic [2]biphenyl-extended pillar[6]arene: Synthesis,controllable self-assembly in water and application in cell-imaging

Synthesis and functionalization of novel macrocyclic host molecules are important topics in supramolecular chemistry. In this work, the first amphiphilic [2]biphenyl-extended pillar[6]arene (AM-[2]BP-ExP6) was designed and synthesized with poly(ethylene glycol) chains as the hydrophilic tails and a rigid cavity as the hydrophobic core. Due to its amphiphilic nature, AM-[2]BP-ExP6 could self-assemble to stable fibers in water. What's more, AM-[2]BP-ExP6 could associate with quaternary ammonium modified tetraphenylethylene guest (QTPE) to form a 2:1 host-guest complex, accompanied by significant enhanced fluorescence. Interestingly, different like AM-[2]BP-ExP6, AM-[2]BP-ExP6⊃QTPE host-guest complex self-assembled into fluorescent particles with diameter about 310 nm, the obtained fluorescent particles can be further employed in living cell imaging.     

A new flavonoid from Cudrania cochinchinensis

Chemical investigation of the ethanol extract of the roots of Cudrania cochinchinensis led to the isolation of a new flavonoid, (6S,12S,13R)-1-methoxy cyanomaclurin (1), together with seven known compounds, 1,3,5-trihydroxy-4-(3′-hydroxy-3′-methylbutyl)xanthone (2), 1,3,6-trihydroxy-4-prenylxanthone (3), 1,3,6,7-tetrahydroxyxanthone (4), 1,3,5,6-tetrahydroxyxanthone (5), 1,3,6-trihydroxy-5-methoxyxanthone (6), resveratrol (7) and oxyresveratrol (8). The structure of compound 1 was elucidated on the basis of 1D and 2D NMR spectra and the HR-ESI-MS data. The absolute stereochemistry was deduced via Rh₂(OCOCF₃)₄-induced CD and NOESY spectra.     

芥子气中毒人员尿液标记物谱分析及其临床诊断应用

该研究基于暴露生物标记物溯源思路,应用于解决芥子气(SM)临床早期诊断、溯源确证难题。建立了芥子气中毒患者尿液中7种游离代谢产物的两步固相萃取/超高效液相色谱-串联质谱(SPE/UPLC-MS/MS)同时定量方法,检出限为5 pg/mL~1 ng/mL,定量下限为10pg/mL~5 ng/mL;结合前期建立的4种游离碱基加合物的同位素稀释-UPLC-MS/MS定量方法,对1例疑似芥子气中毒人员尿液中可能赋存的生物标记物进行了全筛查分析。尿液中共检出3类10种生物标记物,包括首次报道的游离代谢产物芥子亚砜,可确证患者为芥子气中毒;除硫二甘醇外,标记物含量均在暴露后3~4 d达到峰值,随后降低,至7 d仍可检出,其中谷胱甘肽加合物的β裂解产物含量相对较高,可作为芥子气中毒早期诊断与疗效评估的重要指标。     

炸药爆炸作用下地下结构的动力响应分析

基于显式有限元计算程序LS-DYNA3D和粘弹性人工边界条件，建立了爆腔-地下结构-软回填隔震层-岩土介质系统三维弹粘塑性动力响应分析模型，其中爆腔的模拟采用了经验关系式。通过与美陆军技术手册TM5-855-1经验公式的计算结果比较，表明该分析模型与方法是合理的。还进一步讨论了软回填层的隔震效果。     

Nanocomposite of manganese ferrocyanide and graphene: A promising cathode material for rechargeable lithium ion batteries

A nanocomposite of potassium manganese ferrocyanide and graphene (12% C, 88% K_1.8Mn_1.1Fe(CN)₆∙ 0.27H₂O) was prepared by ball milling of graphene oxide powder and nanoparticles of manganese–iron Prussian Blue. It exhibits enhanced electrochemical performance compared to pure Prussian Blue with a specific capacity of 150 mAhg^− 1 at average 3.8 V vs. Li⁺/Li and a good cyclability. The nanocomposite can be considered as competitive to standard cathode materials of present rechargeable lithium ion batteries like cobalt oxide, iron phosphate or NMC.     

含巯基/二硫键聚合物生物材料

含巯基/二硫键聚合物生物材料具有多种良好的性能,作为药物、基因等的释放载体在生物医学领域具有广泛的应用前景。随着基因工程和组织工程的发展,含巯基/二硫键聚合物生物材料的可生物降解性得到高度重视,而怎样改善其降解性能成为限制其应用的关键因素。由于二硫键在细胞外环境里保持稳定,在细胞溶质的还原环境中容易发生断裂,因此在制备新型基因、药物等释放载体上,二硫键充当了重要的角色,它的引入为聚合物生物材料的生物降解性能的设计与改善提供了一条重要的途径。本综述重点以聚合物水凝胶、聚合物微胶束、囊泡等为例,从巯基/烯的光聚合反应、Michael加成反应、氧化还原反应的角度,介绍了巯基/烯在聚合物中形成二硫键的不同途径的研究进展,并详细论述了基因载体、蛋白质载体、小分子药物载体三种还原敏感型材料的制备、表面修饰和改性的进展情况,进一步强调含巯基/二硫键聚合物生物材料的研究在生物医学领域应用的重要性。     

Study on an optical system with coherent laser array source and phase optimization in turbulent atmosphere

Model of an optical system with coherent laser array source and the piston phase optimized by the stochastic parallel gradient descent algorithm is established. With this model, theory of beam propagation through the optical system in turbulent atmosphere is analyzed, and the analytical formulas of the beam average intensity along the propagation path are derived. Strehl ratio of the received beam induced by intensity disorderly distribution and power efficiency of the received beam are introduced to evaluate performance of the optical system. Under the H-V 5/7 atmospheric turbulent model, performance of an optical system with determinate parameters was calculated, and the influences of the propagation distance and the laser wavelength were numerically analyzed, respectively.     

新型喹唑啉类PDE7抑制剂类似物的合成

以邻氨基苯甲酸为原料,经溴代和环合反应合成了4个新型喹唑啉类PDE7抑制剂类似物,其结构经1H NMR和ESI-MS表征。