New 1,3,4-Oxadiazole Derivatives of Pyridothiazine-1,1-Dioxide with Anti-Inflammatory Activity

Numerous studies have confirmed the coexistence of oxidative stress and inflammatory processes. Long-term inflammation and oxidative stress may significantly affect the initiation of the neoplastic transformation process. Here, we describe the synthesis of a new series of Mannich base-type hybrid compounds containing an arylpiperazine residue, 1,3,4-oxadiazole ring, and pyridothiazine-1,1-dioxide core. The synthesis was carried out with the hope that the hybridization of different pharmacophoric molecules would result in a synergistic effect on their anti-inflammatory activity, especially the ability to inhibit cyclooxygenase. The obtained compounds were investigated in terms of their potencies to inhibit cyclooxygenase COX-1 and COX-2 enzymes with the use of the colorimetric inhibitor screening assay. Their antioxidant and cytotoxic effect on normal human dermal fibroblasts (NHDF) was also studied. Strong COX-2 inhibitory activity was observed after the use of TG6 and, especially, TG4. The TG11 compound, as well as reference meloxicam, turned out to be a preferential COX-2 inhibitor. TG12 was, in turn, a non-selective COX inhibitor. A molecular docking study was performed to understand the binding interaction of compounds at the active site of cyclooxygenases.     

基于旋翼负压混合吸附的爬壁清洗机器人系统动力学性能研究

针对爬壁清洗机器人越障时,负压装置的吸附力下降导致吸附不稳定的问题,设计了一种旋翼负压混合吸附工作的多边形履带清洗机器人,并对爬行稳定性及越障性能进行了动力学分析。首先根据机器人爬壁的运动原理,建立机器人沿玻璃幕墙上的动力学模型,计算出电机理论驱动力矩;其次分析机器人在跨越障碍过程中的运动模型,结合与壁面接触的实际受力状态,对越障过程中关键阶段的本体倾翻、滑移两种失效形式进行运动学和动力学分析;然后根据玻璃幕墙实际的障碍高度,确定多边形履带的参数和理论驱动力矩的大小,并研制了实验样机进行爬行和越障试验,结果表明所设计的机器人具有良好的越障性能。     

大数据环境下基于K中心点优化算法的Web服务组合

在当前Web服务海量增加、现有Web服务选择算法低效、用户匹配度差的基础上，针对K中心点算法存在的质点偏移、准确率低和容易发生畸变等问题，提出一种大数据环境下基于K中心点优化算法的Web服务组合方法。该方法是在大数据环境下，根据不同用户需求满意度及Web服务QoS参数，对基于优化初始聚类中心的K中心点算法的Web服务选择及最优Web服务组合进行研究。同时针对不同的选择方法对服务动态选择及组合的准确度、迭代更新次数、候选集选择时间及选择总时间进行实验分析，验证了本文研究方法的有效性和可靠性。     

面向连续查询的敏感语义位置隐私保护方案

针对连续查询位置服务中构造匿名区域未考虑语义位置信息导致敏感隐私泄露问题，通过设计[(K,θ)]-隐私模型，提出一种路网环境下面向连续查询的敏感语义位置隐私保护方案。该方案利用Voronoi图将城市路网预先划分为独立的Voronoi单元，依据用户的移动路径和移动速度，选择具有相似特性的其他[K-1]个用户，构建匿名用户集；利用匿名用户集用户设定的敏感语义位置类型和语义安全阈值，以及用户所处语义位置的Voronoi单元，构建满足[(K,θ)]-隐私模型的语义安全匿名区域，可以同时防止连续查询追踪攻击和语义推断攻击。实验结果表明，与SCPA算法相比，该方案在隐私保护程度上提升约15%，系统开销上降低约20%。     

结合边缘特征先验引导的深度卷积显著性检测

针对当前基于深度学习的显著性检测算法缺少利用先验特征和边缘信息，且在复杂场景中难以检测出鲁棒性强的显著性区域的问题，提出了一种结合边缘特征，利用先验信息引导的全卷积神经网络显著性检测算法。该算法利用三种被经常用到的先验知识结合边缘信息形成先验图，通过注意力机制将提取的先验特征与深度特征有效融合，最终通过提出的循环卷积反馈优化策略迭代地学习改进显著性区域，从而产生更可靠的最终显著图预测。经过实验定性定量分析，对比证明了算法的可靠性。     

Smart work packaging-enabled constraint-free path re-planning for tower crane in prefabricated products assembly process

Lack of constraint-free crane path planning is one of the critical concerns in the dynamic on-site assembly process of prefabrication housing production (PHP). For decades, researchers and practitioners have endeavored to improve both the efficiency and safety of crane path planning from either static environment or re-planning the path when colliding with constraints or periodically updating the path in the dynamic environment. However, there is a lack of approach related to the in-depth exploration of the nature of dynamic constraints so as to assist the crane operators in making adaptive path re-planning decisions by categorizing and prioritizing constraints. To address this issue, this study develops the smart work packaging (SWP)-enabled constraints optimization service. This service embraces the core characteristics of SWP, including adaptivity, sociability, and autonomy to achieve autonomous initial path planning, networked constraints classification, and adaptive decisions on path re-planning. This service is simulated and verified in the BIM environment, and it is found that SWP-enabled constraints optimization service can generate the constraint-free path when it is necessary.     

Modeling and design of 3-D MPPT for ultra low power RF energy harvesters

Radio-Frequency (RF) energy harvesting must cope with the limited availability and high variability of the energy source. In this paper, the modeling of an RF harvester for ultra low power environments is presented. A mathematical model based on theoretical analysis is developed. The model demonstrates that the maximum transferred power point is located in a three-dimensional space defined by the input capacitance, the output voltage, and the load resistance of the rectifier circuit. Moreover, the mathematical model returns results in substantial agreement with the SPICE simulation results, while guaranteeing a remarkable reduction of the required computation time. Furthermore, the paper reports the implementation of a mixed signal system for the 3-D MPPT, to be embedded in an RF harvester, in a 65 nm CMOS technology. The circuit exhibits a simulated power consumption lower than 100 nW, making this solution suitable for ultra low power harvesting.     

高强不锈钢绞线网与ECC黏结-滑移关系模型

高强不锈钢绞线网与ECC的黏结是二者协同工作的基础，且黏结 滑移关系模型是其黏结性能的综合反映，故通过对17组51个高强不锈钢绞网增强ECC薄板试件进行单边拉拔试验，研究横向钢绞线间距、纵向钢绞线直径和相对锚固长度等因素对钢绞线网在ECC中黏结性能的影响规律。试验结果表明，横向钢绞线的设置可使黏结破坏由脆性破坏转变为延性破坏；高强不锈钢绞线网与ECC的黏结滑移曲线可分为5个阶段，分别为上升段、微降段、延性强化段、下降段和残余段。基于试验结果，对钢绞线网在ECC中的黏结破坏特征和黏结 滑移机理进行分析，在相关黏结-滑移关系模型的基础上，提出钢绞线网与ECC的黏结 滑移关系模型，并进行模型参数分析。所提模型及模型参数计算公式与试验结果吻合良好，能较好地反映钢绞线网与ECC的界面黏结滑移特征。     

基于BIM技术和有限元的检测与分析在PC结构中的应用研究

本文建立了PC结构施工全过程的BIM模型及有限元分析模型,对施工过程进行数值模拟与动态、静态监测,对装配式结构进行了结构性能评价,为结构可视化施工监测提供了技术支持。     

Unusual Two-Step Assembly of a Minimalistic Dipeptide-Based Functional Hypergelator

Self-assembled peptide hydrogels represent the realization of peptide nanotechnology into biomedical products. There is a continuous quest to identify the simplest building blocks and optimize their critical gelation concentration (CGC). Herein, a minimalistic, de novo dipeptide, Fmoc-Lys(Fmoc)-Asp, as an hydrogelator with the lowest CGC ever reported, almost fourfold lower as compared to that of a large hexadecapeptide previously described, is reported. The dipeptide self-assembles through an unusual and unprecedented two-step process as elucidated by solid-state NMR and molecular dynamics simulation. The hydrogel is cytocompatible and supports 2D/3D cell growth. Conductive composite gels composed of Fmoc-Lys(Fmoc)-Asp and a conductive polymer exhibit excellent DNA binding. Fmoc-Lys(Fmoc)-Asp exhibits the lowest CGC and highest mechanical properties when compared to a library of dipeptide analogues, thus validating the uniqueness of the molecular design which confers useful properties for various potential applications.