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.     

A carbonyl-rich covalent organic framework as a high-performance cathode material for aqueous rechargeable zinc-ion batteries

Aqueous rechargeable zinc-ion batteries (ZIBs) provide high theoretical capacity, operational safety, low-cost and environmental friendliness for large-scale energy storage and wearable electronic devices, but their future development is plagued by low capacity and poor cycle life due to the lack of suitable cathode materials. In this work, a covalent organic framework (Tp-PTO-COF) with multiple carbonyl active sites is synthesized and successfully introduced in aqueous rechargeable ZIBs for the first time. Tp-PTO-COF delivers high specific capacities of 301.4 and 192.8 mA h g⁻¹ at current densities of 0.2 and 5 A g⁻¹, respectively, along with long-term durability and flat charge–discharge plateaus. The remarkable electrochemical performance is attributed to the abundance of nucleophilic carbonyl active sites, well defined porous structure and inherent chemical stability of Tp-PTO-COF. Moreover, the structural evolution and Zn²⁺ ion intercalation mechanism are discussed and revealed by the experimental analysis and density functional theory calculations. These results highlight a new avenue to develop organic cathode materials for high performance and sustainable aqueous rechargeable ZIBs.

A covalent organic framework (Tp-PTO-COF) with carbonyl active sites was proposed as a novel cathode material and successfully applied in aqueous rechargeable zinc-ion batteries (ZIBs).     

Ultranarrow bandwidth Faraday atomic filter approaching natural linewidth based on cold atoms

An ultranarrow bandwidth Faraday atomic filter is realized based on cold ~(87)Rb atoms. The atomic filter operates at 780 nm on the 5~2 S_(1/2), F = 2 to 5~2 P_(3/2), F'= 3 transition with a bandwidth of 7.1(8) MHz, which is approaching the natural linewidth of the transition. The peak transmission achieves 2.6(3)% by the multi-pass probe method. This atomic filter based on cold atoms may find potential applications in self-stabilizing lasers in the future.     

聚合物纳米孔隙增透膜制备工艺的研究

论述了聚合物纳米孔隙增透膜的制备工艺流程,分析了聚合物材料分子量、实验环境温度和湿度、溶剂挥发性等条件对纳米孔隙增透膜的影响。研究表明,聚合物材料分子量的增大、温度的降低、湿度的升高以及采用挥发性弱的溶剂都将导致增透膜孔隙尺寸的增大,孔隙越大其对光的散射损耗就会增大,所以增透膜的透过率就越低。通过大量的试验分析得出一组较理想的工艺参量:使用低分子量的聚合物材料(小于15 kg/mol),环境温度大于25℃、环境相对湿度小于30%,在采用低沸点的溶剂如四氢呋喃等措施下可有效降低增透膜散射损耗。     

基于光子数目比较的激光测距法

提出了一种新颖的激光测距方法。该方法避开了传统激光测距法中使用复杂辅助电子设备对脉冲计时或比较相位差的过程,而主要通过光学手段分析和提取待测距离信息,最终通过比较大量光子数目的方法求得待测距离。并利用单轴晶体的双折射和全内双反射性质,用特殊结构的单块LiNbO3晶体设计了实施该方法的主体装置。结果表明,该激光测距法同目前普遍使用的激光测距法相比,不但简化了结构,而且有很高的测距精度,从而为激光测距开拓了一种新的思路。     

Discovering Phase Field Models from Image Data with the Pseudo-Spectral Physics Informed Neural Networks

In this paper,we introduce a new deep learning framework for discovering the phase-field models from existing image data.The new framework embraces the approxim...     

The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics,Tissue Distribution,Excretion, and Metabolism of β-Cyclodextrin in Rats

β-cyclodextrin has a unique annular hollow ultrastructure that allows encapsulation of various poorly water-soluble drugs in the resulting cavity, thereby increasing drug stability. As a bioactive molecule, the metabolism of β-cyclodextrin is mainly completed by the flora in the colon, which can interact with API. In this study, understanding the in vivo fate of β-cyclodextrin, a LC-MS/MS method was developed to facilitate simultaneous quantitative analysis of pharmaceutical excipient β-cyclodextrin and API dextromethorphan hydrobromide. The established method had been effectively used to study the pharmacokinetics, tissue distribution, excretion, and metabolism of β-cyclodextrin after oral administration in rats. Results showed that β-cyclodextrin was almost wholly removed from rat plasma within 36 h, and high concentrations of β-cyclodextrin distributed hastily to organs with increased blood flow velocities such as the spleen, liver, and kidney after administration. The excretion of intact β-cyclodextrin to urine and feces was lower than the administration dose. It can be speculated that β-cyclodextrin metabolized to maltodextrin, which was further metabolized, absorbed, and eventually discharged in the form of CO₂ and H₂O. Results proved that β-cyclodextrin, with relative low accumulation in the body, had good safety. The results will assist further study of the design and safety evaluation of adjuvant β-cyclodextrin and promote its clinical development.     

Discovery of Novel Non-Oxime Reactivators Showing In Vivo Antidotal Efficiency for Sarin Poisoned Mice

A family of novel efficient non-oxime compounds exhibited promising reactivation efficacy for VX and sarin inhibited human acetylcholinesterase was discovered. It was found that aromatic groups coupled to Mannich phenols and the introduction of imidazole to the ortho position of phenols would dramatically enhance reactivation efficiency. Moreover, the in vivo experiment was conducted, and the results demonstrated that Mannich phenol L10R1 (30 mg/kg, ip) could afford 100% 48 h survival for mice of 2*LD₅₀ sarin exposure, which is promising for the development of non-oxime reactivators with central efficiency.     

1200 V碳化硅功率MOSFET低温特性的实验表征及分析

碳化硅功率MOSFET是宽禁带功率半导体器件的典型代表,具有优异的电气性能。基于低温环境下的应用需求,研究了1200 V碳化硅功率MOSFET在77.7 K至300 K温区的静/动态特性,定性分析了温度对碳化硅功率MOSFET性能的影响。实验结果显示,温度从300 K降低至77.7 K时,阈值电压上升177.24%,漏-源极击穿电压降低32.99%,栅极泄漏电流降低82.51%,导通电阻升高1142.28%,零栅压漏电流降低89.84%(300 K至125 K)。双脉冲测试显示,开通时间增大8.59%,关断时间降低16.86%,开关损耗增加48%。分析发现,碳化硅功率MOSFET较高的界面态密度和较差的沟道迁移率,是导致其在低温下性能劣化的主要原因。     

Adaptive vehicle posture and height synchronization control of active air suspension systems with multiple uncertainties

This paper addresses the tasks of height and posture motion control for an electronically controlled active air suspension (AAS) system. A mathematical model of a vehicle body with AAS system is established to describe the dynamic characteristics and then formulated into a multi-input multi-output nonlinear system by considering parametric uncertainties and unmodelled dynamics. Based on this mathematical model, a synchronization control strategy is proposed to adjust the heights of adjacent AASs simultaneously, driving the pitch and roll angles closely to an arbitrarily neighborhood of zero, achieving global uniform ultimate boundedness. The proposed controller is robust to parametric uncertainties and external disturbances. A projection operator is utilized to limit the estimated parameters to their corresponding prescribed bounds in finite time. A co-simulation is conducted by combining a virtual vehicle plant with ASS system in AMEsim with the proposed synchronization controller in MATLAB/Simulink. Simulation results demonstrate that the proposed synchronization controller is effective and robust.