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Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase

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Acta Pharmaceutica Sinica B 2016年第1期6卷 32-45页

作者： Yu zhou Jun liu Mingyue zheng Shuli zheng Chunyi Jiang Xiaomei zhou Dong Zhang Jihui Zhao Deju Ye Mingfang zheng Hualiang Jiang Dongxiang liu Jian Cheng Hong liu CAS Key Laboratory of Receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences China Pharmaceutical University Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and Institute of Neuroscience Soochow University

Human 5-lipoxygenase (5-LOX) is a well-validated drug target and its inhibitors are potential drugs for treating leukotriene-related disorders. Our previous work on structural optimization of the hit compound 2 from our in-house collection identified two lead compounds, 3a and 3b, exhibiting a potent inhibitory profile against 5-LOX with IC50 values less than 1 mu mol/L in cell-based assays. Here, we further optimized these compounds to prepare a class of novel pyrazole derivatives by opening the fused ring system. Several new compounds exhibited more potent inhibitory activity than the lead compounds against 5-LOX. In particular, compound 4e not only suppressed lipopolysaccharide-induced inflammation in brain inflammatory cells and protected neurons from oxidative toxicity, but also significantly decreased infarct damage in a mouse model of cerebral ischemia. Molecular docking analysis further confirmed the consistency of our theoretical results and experimental data. In conclusion, the excellent in vitro and in vivo inhibitory activities of these compounds against 5-LOX suggested that these novel chemical structures have a promising therapeutic potential to treat leukotriene-related disorders. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

关键词： 5-Lipoxygenase 5-LOX inhibitors Pyrazole derivatives Leukotrienes-related diseases In vivo Benzo-fuse heterocyle Ischemic incults Brain inflammation

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A broad learning-based comprehensive defence against SSDP reflection attacks in IoTs

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Digital Communications and Networks 2023年第5期9卷 1180-1189页

作者： Xin liu Liang zheng Sumi Helal Weishan Zhang Chunfu Jia Jiehan zhou College of Computer Science and Technology China University of Petroleum(East China)QingdaoChina School of Computing Lancaster University UK Nankai University TianjinChina Information Technology and Electrical Engineering University of OuluFinland

The proliferation of Internet of Things(IoT)rapidly increases the possiblities of Simple Service Discovery Protocol(SSDP)reflection *** DDoS attack defence strategies deploy only to a certain type of devices in the attack chain,and need to detect attacks in advance,and the detection of DDoS attacks often uses heavy algorithms consuming lots of computing *** paper proposes a comprehensive DDoS attack defence approach which combines broad learning and a set of defence strategies against SSDP attacks,called Broad Learning based Comprehensive Defence(BLCD).The defence strategies work along the attack chain,starting from attack sources to *** defends against attacks without detecting attacks or identifying the roles of IoT devices in SSDP reflection *** also detects suspicious traffic at bots,service providers and victims by using broad learning,and the detection results are used as the basis for automatically deploying defence strategies which can significantly reduce DDoS *** evaluations,we thoroughly analyze attack traffic when deploying BLCD to different defence *** show that BLCD can reduce the number of packets received at the victim to 39 without affecting the standard SSDP service,and detect malicious packets with an accuracy of 99.99%.

关键词： Denial-of-service DRDoS SSDP reflection Attack Broad learning Traffic detection

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Numerical Simulation for Arc Windshields of Aircrafts Subjected to Bird Impact

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上海交通大学学报 2004年第z2期38卷 147-151页

作者： Yao Xiaohu Zhao Longmao liu xiaoming Institute of Applied Mechanics Taiyuan University of Technology China College of Traffic and Communications South China University of Technology China Institute of Applied Mechanics Taiyuan University of Technology China Chengdu Aircraft Industry Company China

A finite element model including full-scale circular arc windshield glass and the relative parts of the military plane is established in this paper. The model is analyzed by using an explicit element code LS-DYNA3D for analyzing the nonlinear dynamic response of structures. The data in aspects of displacement, strain, stress and contact force in the process of deformation are obtained. The deformation and failure mechanism of circular arc windshield glass are discussed. The possible location at which failure may take place is given. The valuable data are provided for designing,researching and producing new windshields with high crashworthiness.

关键词： bird impact arc windshield dynamic response liquid-solid coupling

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New Non-TravellingWave Solutions of Calogero Equation

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Advances in Applied Mathematics and Mechanics 2016年第6期8卷 1036-1049页

作者： xiaoming Peng Yadong Shang Xiaoxiao zheng School of Mathematics and Information Science Guangzhou UniversityGuangzhou 510006China Key Laboratory of Mathematics and Interdisciplinary Sciences of Guangdong Higher Education Institutes Guangzhou UniversityGuangzhou 510006China

In this paper,the idea of a combination of variable separation approach and the extended homoclinic test approach is proposed to seek non-travelling wave solutions of Calogero *** equation is reduced to some(1+1)-dimensional nonlinear equations by applying the variable separation approach and solves reduced equations with the extended homoclinic test *** on this idea and with the aid of symbolic computation,some new explicit solutions can be obtained.

关键词： Variable separation approach extended homoclinic test approach non-travelling wave solution.

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Distributed order estimation for continuous-time stochastic systems

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Control Theory and Technology 2024年第3期22卷 406-418页

作者： Xinghua Zhu Zhixin liu xiaoming Hu Key Laboratory of Systems and Control Academy of Mathematics and Systems ScienceBeijing 100190China School of Mathematical Sciences University of Chinese Academy of SciencesBeijing 100190China Department of Mathematics KTH Royal Institute of TechnologyStockholm 10044Sweden

In this paper,we investigate the distributed estimation problem of continuous-time stochastic dynamic systems over sensor networks when both the system order and parameters are *** propose a local information criterion(LIC)based on the L_(0)penalty *** minimizing LIC at the diffusion time instant and utilizing the continuous-time diffusion least squares algorithm,we obtain a distributed estimation algorithm to simultaneously estimate the unknown order and the parameters of the *** dealing with the effect of the system noises and the coupling relationship between estimation of system orders and parameters,we establish the almost sure convergence results of the proposed distributed estimation ***,we give a simulation example to verify the effectiveness of the distributed algorithm in estimating the system order and parameters.

关键词： Stochastic differential equations Sensor networks Distributed order estimation Cooperative excitation condition.Convergence

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Unearthing old rice germplasm,illuminating a new way to improvement

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Journal of Integrative Plant Biology 2024年第6期66卷 1041-1043页

作者： xiaoming zheng Ramaiah Venuprasad Ajay Kohli International Rice Research Institute Metro ManilaPhilippines

We are on the cusp of a new era,with the global pop-ulation surpassing 8 billion,and over half relying on riceas their staple food(Sasaki and Burr,2000).Despite thisgrowing demand,rice yield per unit has seemingly plateauedfor many years(Song et al.,2022).This stagnation raisesserious concerns about future global food security,especiallyconsidering the shrinking arable land in many countries.

关键词： germplasm plateau spite

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Architecture for Cellular Enabled Integrated Communication and Sensing Services

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China Communications 2023年第9期20卷 59-77页

作者： Bo liu Qixun Zhang zheng Jiang Dongsheng Xue Chenlong Xu Bowen Wang xiaoming She Jinlin Peng School of Information and Communication Engineering Beijing University of Posts and TelecommunicationsBeijing 100876China China Telecom Corporation Limited Beijing Research Institute Beijing 102209China Artificial Intelligence Research Center National Innovation Institute of Defense TechnologyBeijingChina

There is growing interest in the integrated sensing and communication(ISAC)to extend the 5G+/6G network capabilities by introducing sensing *** the solutions for mono-static or bi-static ISAC have shown feasibility and benefits based on existing 5G physical layer design,whether and how to coordinate multiple ISAC devices to better exert networking performance are rarely discussed.3 rd Partnership Project(3GPP)has initiated the ISAC use cases study,and the follow-up studies for network architecture could be *** this article,we focus on gNB-based sensing mode and propose ISAC functional framework with given of highlevel service procedures to enable cellular based ISAC *** the proposed ISAC framework,three types of network functions for sensing service as Sensing Function(SF),lightweight-Edge Sensing Function(ESF)and full-version-ESF are designed with interaction with network nodes to fulfill the latency requirements of ISAC use ***,with simulation evaluations and hardware testbed results,we further verify the performance benefit and feasibility to enable ISAC in 5G for the gNB-based sensing mode with new design on SF and related signaling protocols.

关键词： integrated sensing and communication(ISAC) network architecture 5G system

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A new scheme of climate-vegetation regionalization in the Hengduan Mountains Region

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Science China Earth Sciences 2024年第3期67卷 751-768页

作者： Xueqin ZHANG xiaoming XU Xiang LI Peng CUI Du zheng Key Laboratory of Land Surface Pattern and Simulation Institute of Geographic Sciences and Natural Resources ResearchChinese Academy of SciencesBeijing 100101China University of Chinese Academy of Sciences Beijing 100049China China-Pakistan Joint Research Center on Earth Sciences Chinese Academy of Sciences-Higher Education Commission of PakistanIslamabad 45320Pakistan

The Hengduan Mountains Region(HMR) is essential for the future ecological protection, clean energy production,Sichuan-Xizang and Yunnan-Xizang railways, and other major infrastructure projects in China. The distributions of climate and vegetation exhibit significant regional differentiation and vertical zonality due to the rugged longitudinal ranges and gorges and the complex disaster-prone environments in HMR. Therefore, it is urgent to develop the climate-vegetation regionalization in HMR to effectively satisfy the national requirements such as agricultural production and ecological protection, mountain disaster risk prevention, and major project construction. We here develop a new scheme of climate-vegetation regionalization with the latest demarcation outcome of HMR, the ground observation from 122 meteorological stations in HMR and its surrounding areas during 1990–2019, and the high-precision remote sensing data of land cover types. The new scheme first constructs the regionalization index system, fully considering the extraordinarily complicated geomorphic pattern of mountains and valleys, the scarcity of meteorological observations, and the remarkable differentiation of climate and vegetation in HMR. The system consists of three primary regionalization indices(i.e., days with daily average temperature steady above 10°C, aridity index, and main vegetation types, dividing the temperature zones, moisture regions, and vegetation subregions, respectively) and three auxiliary indices of the accumulated temperature above 10°C, and the temperatures in January and July. Then, the HMR is divided into five temperature zones, 20 moisture regions, and 55 vegetation subregions. Compared with previous regionalization schemes, the new scheme optimizes the climate spatial interpolation model of thin plate smoothing spline suitable for the unique terrain in HMR. Moreover, the disputed division index threshold between different climatic zones(regions) is scientifically clarifi

关键词： Climate-vegetation regionalization Thin plate smoothing spline(TPSS) GeoDetector Stepwise downscaling pane division method Hengduan Mountains Region

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Engineering nanointerface of molybdenum-based heterostructures to boost the electrocatalytic hydrogen evolution reaction

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Journal of Energy Chemistry 2021年第7期30卷 370-376页

作者： Tong liu Shuqing zhou Jing Qi Kaiwen Wang Lirong zheng Qingming Huang Tianhua zhou Jian Zhang State Key Laboratory of Structural Chemistry Fujian Institute of Research on the Structure of MatterChinese Academy of SciencesFuzhou 350002FujianChina School of Physical Science and Technology ShanghaiTech UniversityShanghai 201210China Key Laboratory of Applied Surface and Colloid Chemistry Ministry of EducationSchool of Chemistry and Chemical EngineeringShaanxi Normal UniversityXi’an 710000ShaanxiChina Beijing Key Laboratory and Institute of Microstructure and Property of Advanced Materials Beijing University of TechnologyBeijing 100124China Beijing Synchrotron Radiation Facility(BSRF) Institute of High Energy PhysicsChinese Academy of SciencesBeijing 100049China Testing Center Fuzhou UniversityFuzhou 350116FujianChina

Rational heterostructure-design in electrocatalysts represents a promising approach toward high performance in the electrocatalytic hydrogen evolution reaction(HER).In specific,optimizing the H adsorption behavior at the surface/interface of heterostructure is of key importance to improve the catalytic ***,we demonstrate the construction of a heterostructure from a well-defined oxygenbridged Co/Mo heterometallic zeolitic imidazolate framework(MOZ) as an efficient electrocatalyst for *** optimized hybrid exhibits high catalytic activity and stability in electrolytes with a wide pH *** XPS,XAS and theoretical studies reveal that the regulation of metal species can tailor the lattice of Mo_(2)C within the hybrid and induce the formation of defect sites,which could not only induce surface charge transfer between the atoms and provide an additional active site,but also affect the H adsorption behavior at the interface of a *** work provides an effective strategy to design a heterostructure with tailored active sites for energy conversion.

关键词： Electrocatalysis Metal-organic framework Water splitting Heterostructure

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Cycle performance of Cu-based oxygen carrier based on a chemical-looping combustion process

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Journal of Energy Chemistry 2016年第1期25卷 101-109页

作者： xiaoming zheng Lixin Che Yanqiong Hao Qingquan Su School of Mechanical Engineering University of Science and Technology Beijing Beijing 100083 China Beijing Gas Group Research Institute Beijing 100011 China Beijing Engineering Research Center for Energy Saving and Environmental Protection University of Science and Technology Beijing Beijing 100083 China

The cycle life of oxygen carrier（OC） is crucial to the practical applications of chemical looping combustion（CLC）. Cycle performance of Cu/SiO2 prepared with a mechanical mixing method was evaluated based on a CLC process characterized with an added methane steam reforming step. The Cu/SiO2 exhibited high redox reactivity in the initial cycles, while the performance degraded with cycle number. Through characterization of the degraded Cu/SiO2, the performance degradation was mainly caused by the secondary particles＇ fragmentation and the fine particles＇ local agglomeration, which worsened the distribution and diffusion of the reactive gases in the packed bed. A regeneration method of the degraded OC based on re-granulation has been proposed, and its mechanism has been illustrated. With this method, the performance of the degraded OC through 420 redox cycles was recovered to a level close to the initial one.

关键词： Chemical-looping combustion Cu-based oxygen carrier Cycle life

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