Design,Synthesis, and Structure–Activity Relationship Study of Potent MAPK11 Inhibitors

Huntington’s disease (HD) is a rare single-gene neurodegenerative disease, which can only be treated symptomatically. Currently, there are no approved drugs for HD on the market. Studies have found that MAPK11 can serve as a potential therapeutic target for HD. Regrettably, no MAPK11 small molecule inhibitors have been approved at present. This paper presents three series of compounds that were designed and synthesized based on the structure of skepinone-L, a known MAPK14 inhibitor. Among the synthesized compounds, 13a and 13b, with IC₅₀ values of 6.40 nM and 4.20 nM, respectively, displayed the best inhibitory activities against MAPK11. Furthermore, the structure–activity relationship (SAR) is discussed in detail, which is constructive in optimizing the MAPK11 inhibitors for better activity and effect against HD.     

低压供热涂层材料制备及热性能研究

低压供热技术具有安全系数高和节能降耗等优势,因而成为石化稠油长输管线、风力发电叶片冬季防覆冰和室内供暖等领域的研究热点之一。本文制备了一系列低压供热涂层材料,研究不同碳功能填料对涂层发热速率、发热功率及最高发热温度的影响规律,并揭示石墨烯和碳纤维对提升涂层材料热性能的协同作用。其中石墨烯纳米片的还原程度对材料热性能具有重要影响,降低其表面官能团密度对提升涂层供热特性具有促进作用,但是官能团密度过低会导致石墨烯纳米片的团聚现象,引起涂层发热不均匀。加入适量碳纤维可以提高石墨烯的均匀分散性,提升发热速率。优化石墨烯纳米片和碳纤维的比例后,采用24V电压驱动时,涂层材料的发热速率达到7.1℃·s^-1,功率密度为800W·m^-2,最高发热温度为124℃。     

A Novel 3D Na(I) Coordination Polymer Constructed by 3,5-Bis(4'-Carboxy-Phenyl)-1,2,4-Triazole: Synthesis,Crystal Structure,and Photocatalytic Property

Crystallography Reports - A novel 3D metal coordination polymer, {[Na4(µ2-H2O)(DMF)2(BCT)2]?DMF}n (I) (DMF = N,N-dimethylformamide, H2BCT =...     

The reaction of allyldialkyltelluronium bromides with anilines

Allyldialkyltelluronium bromides were treated with aromatic amines in 1,2-dichloroethane, readily giving allyl aryl amines in excellent yields.     

对正负一级能量之比测量光栅参量方法的改进

提出利用同一波长的入射光在双面入射时两个能量之比的比值对光栅的参量进行测量,进一步提高准确度。首先从理论上比较正弦面形光栅在单一面入射及双面入射时各种衍射效率对光栅表面粗糙度的敏感程度;然后模拟测量出该正弦面型光栅在双面入射情况下的光栅参量;最后成功反演出体积相位全息光栅的三个参量,其测量结果为0.080μm,1.452μm,20.5μm准确度比单一入射面情况(0.080μm,1.451μm,20.1μm)时要高。同时该法继承了原来方法的无损伤、操作简便、可重复、易推广、成本低等优点。     

Thermal Conductance of Graphene-Titanium Interface: A Molecular Simulation

Titanium is a commonly used material in aviation, aerospace, and military applications, due to the outstanding mechanical properties of titanium and its alloys. However, its relatively low thermal conductivity restricts its extended usage. The use of graphene as a filler shows great potential for the enhancement of thermal conductivity in titanium-based metal-matrix composites (MMCs). We used classical molecular dynamics (MD) simulation methods to explore the thermal conductance at the titanium–graphene (Ti/Gr) interface for its thermal boundary conductance, which plays an important role in the thermal properties of Ti-based MMCs. The effects of system size, layer number, temperature, and strain were considered. The results show that the thermal boundary conductance (TBC) decreases with an increasing layer number and reaches a plateau at n = 5. TBC falls under tensile strain and, in turn, it grows with compressive strain. The variation of TBC is explained qualitatively by the interfacial atomic vibration coupling factor. Our findings also provide insights into ways to optimize future thermal management based on Ti-based MMCs materials.     

On the Interfacial Flow Over Porous Media Composed of Packed Spheres: Part 1-Identification of the Effective Slip Length

Transport in Porous Media - The effective slip length at the interface between pure fluid flow and porous media composed of packed spheres has been accurately characterized. In this study, as the...     

Nonlinear vibration effects on the fatigue life of fluid-conveying pipes composed of axially functionally graded materials

Nonlinear Dynamics - Fatigue is inevitable in pipes conveying fluid due to unwanted vibration. Internal resonance occurs in such pipes due to pre-pressure. For the first time, the effects of...     

Robust fixed-time attitude stabilization control of flexible spacecraft with actuator uncertainty

Nonlinear Dynamics - A robust fixed-time control framework is presented to stabilize flexible spacecraft’s attitude system with external disturbance, uncertain parameters of inertia, and...