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Design,synthesis,and biological evaluation of 1,2,4-triazole derivatives as potent antitubercular agents

Chinese Chemical Letters 2024年第3期35卷 326-331页

作者： Yu Wen Shichun Lun Yuxue Jiao Wei Zhang Tianyu Hu Ting Liu Fan Yang Jie Tang Bing Zhang william R.Bishai Li-Fang Yu Shanghai engineering Research Center of Molecular Therapeutics and New Drug Development School of Chemistry and Molecular EngineeringEast China Normal UniversityShanghai 200062China Center for Tuberculosis Research Department of MedicineDivision of Infectious DiseaseJohns Hopkins School of MedicineBaltimoreMD21231-1044United States Shanghai Institute for Advanced Immunochemical Studies and School of Life Science and Technology ShanghaiTech UniversityShanghai 201210China Shanghai Key Laboratory of Green Chemistry and Chemical Process School of Chemistry and Molecular EngineeringEast China Normal UniversityShanghai 200062China

Inhibition of mycobacterial membrane protein large 3(MmpL3)thereby affecting the mycolic acid biosynthetic pathway has been proven to be an effective strategy for developing antitubercular *** on the X-ray crystal structure of MmpL3 inhibitor complexes,a series of novel 1,2,4-triazole derivatives were designed,synthesized and evaluated antitubercular activity against Mtb strain *** structure–activity relationship exploration resulted in the identification of compounds 21 and 28,which possess potent antitubercular activity against Mtb strain H37Rv[minimum inhibitory concentration(MIC)=0.03–0.13μg/mL]and the clinical isolates of multidrug resistance(MDR)and extensive drug resistance(XDR)tuberculosis(MIC=0.06–1.0μg/mL).Moreover,compounds 21 and 28 showed neglectable cytotoxicity(IC_(50)≥32μg/mL)to the mammalian Vero cells and favorable physicochemical and pharmacokinetic properties according to the in silico absorption,distribution,metabolism and excretion(ADMe)***,the potential target of representative 1,2,4-triazole 28 was identified to be MmpL3 using a microscale thermophoresis(MST)assay.

关键词： Tuberculosis MDR and XDR-TB MmpL3 inhibitor 1 2 4-Triazole Structure-based drug design

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Sustainable plasticulture in Chinese agriculture: a review of challenges and routes to achieving long-term food and ecosecurity

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Frontiers of Agricultural Science and engineering 2024年第1期11卷 155-168页

作者： Samuel J.CUSWORTH william J.DAVIeS Martin R.MCAINSH Carly J.STeVeNS Weilu WANG Lancaster environment Centre Lancaster UniversityLancasterLA14YQUK The Institutes of Agricultural Science and Technology Development Yangzhou UniversityYangzhou 225009China

Plastic pollution is global concern, affecting most aspects of global food production systems. Plasticulture, a practice used in agriculture to improve crop quality and quantity, among other factors, is a significant source of plastic pollution. This review examines the extent of plasticulture in China, the implications of the practice across decades of use and the legislative instruments used to resolve those issues. It briefly assesses the effectiveness of these policies and proposes possible future innovations to promote increases in long-term food and eco-security, where sustainable plasticulture is a key agent for change. While plasticulture has increased agricultural productivity in growth-limiting conditions, plastic pollution in agricultural soils has become acute in China. Consequently, plastic pollution is having deleterious effects on soil health and in turn, crop productivity in China. Plastic pollution in agriculture is a multifaceted issue and so proposed solutions should be informed by this complexity. Current measures do not reflect a holistic approach to solving this socioecological challenge and adopt a top-down approach, with little or no supportive mechanisms. Future recommendations need to consider the particular set of conditions that influence the production, use and end-of-life management of agriplastics,specific to the environmental, economic and social conditions in each location.

关键词： Circular plastics economy crop production food security plastic pollution sustainable plasticulture

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Coordinating environmental protection and agricultural development: a village-based case study for promoting green transformation

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Frontiers of Agricultural Science and engineering 2024年第1期11卷 100-112页

作者： Kemo JIN Nico HeeRINK william JDAVIeS Jianbo SHeN Yifeitong ZHANG Yong HOU Yaqiao ZHAO Zhengxiong ZHAO Fusuo ZHANG State Key Laboratory of Nutrient Use and Management College of Resources and Environmental SciencesChina Agricultural UniversityBeijing 100193China Department of Social Sciences Wageningen University and Research6700 AA Wageningenthe Netherlands Lancaster environment Centre University of LancasterLancasterLA14YQUK College of Agricultural and environmental science University of CaliforniaDavisCA 95616USA College of economics and Management Yunnan Agricultural UniversityKunming 650201China College of Resources and environment Yunnan Agricultural UniversityKunming 650201China

Balancing ecological preservation with sustainable agricultural practices is a global issue. erhai Lake has felt this challenge keenly. To address it, in 2022, a Science and Technology Backyards(STBs) project was launched in Gusheng Village. The goal of this is to care for the environment while ensuring that farms and farmers can thrive sustainably. The uniqueness of the erhai STB arises from its interdisciplinary integration, encompassing fields such as ecology, agronomy and social science, resulting in specifically-designed solutions for the erhai context. While this model aligns with broader STB paradigms, its distinctive edge lies in technological innovation and robust support mechanisms for local agricultural stakeholders. This paper describes the methodology and outcomes of the STB initiative, highlighting its pivotal role in spearheading sustainable transition in erhai. Preliminary findings underscore the potential of the STB model as an efficacious tool for harmonizing environmental conservation and agricultural practices, that are both financially and environmentally sustainable, rendering it a potential model for comparable regions in China and other counties.

关键词： Agriculture green development Science and Technology Backyards erhai environmental protection smallholders

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Fuel cell stack design and modelling with a double-stage boost converter coupled to a single-phase inverter

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CLeAN eNeRGY 2024年第1期8卷 188-196页

作者： elnagi, Basem e. Ismaiel, Ahmed M. Mansour, Hany S. e. Abd-Alwahab, M. N. Suez Canal Univ Fac Engn Elect Engn Dept Ismailia 41522 Egypt

A comprehensive proton-exchange membrane fuel cell stack model was developed and integrated with a two-stage DC/DC boost converter. It was directly coupled to a single-phase (two levels-four pulses) inverter without a transformer. The pulse-width modulation signal was used to independently regulate every converter phase. The converter was modelled using a MATLAB (R)/Simulink (R) environment and an appropriate voltage control method. The analysis features of the suggested circuit were created and, through established experiments, the simulation results were verified. A single-phase (two levels-four pulses) inverter control circuit was tested and it produced a pure sinusoidal waveform with voltage control. It matches the voltage of the network in terms of amplitude and frequency. A sinusoidal pulse-width modulation approach was performed using a single-phase (two levels-four pulses) pulse-width modulation inverter. The results demonstrated an enhancement in the standard of the output wave and tuned the dead time with a reduction of 63 mu s compared with 180 mu s in conventional techniques. A comprehensive model of a proton-exchange membrane fuel cell stack is integrated with a single-phase (two levels-four pulses) inverter without a transformer. Pulse-width modulation is used to independently regulate every converter phase. As a result, the dead time is reduced compared to conventional techniques. Graphical Abstract

关键词： PeM fuel cell pulse-width modulation single-phase inverter and double-stage DC/DC boost converter PeRFORMANCe SYSTeM

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Respiratory protein-driven selectivity during the Permian-Triassic mass extinction

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The Innovation 2024年第3期5卷 122-128页

作者： Haijun Song Yuyang Wu Xu Dai Jacopo Dal Corso Fengyu Wang Yan Feng Daoliang Chu Li Tian Huyue Song william JFoster State Key Laboratory of Biogeology and environmental Geology School of Earth SciencesChina University of GeosciencesWuhan 430074China Biogéosciences UMR 6282CNRSUniversitéde Bourgogne21000 DijonFrance Universitat Hamburg Institute for Geology20148 HamburgGermany

extinction selectivity determines the direction of macroevolution,especially during mass extinction;however,its driving mechanisms remain poorly *** investigating the physiological selectivity of marine animals during the Permian-Triassic mass extinction,we found that marine clades with lower O2-carrying capacity hemerythrin proteins and those relying on O2 diffusion experienced significantly greater extinction intensity and body-size reduction than those with higher O2-carrying capacity hemoglobin or hemocyanin *** findings suggest that animals with high O2-carrying capacity obtained the necessary O2 even under hypoxia and compensated for the increased energy requirements caused by ocean acidification,which enabled their survival during the Permian-Triassic mass ***,high O2-carrying capacity may have been crucial for the transition from the Paleozoic to the Modern evolutionary Fauna.

关键词： extinction selectivity finding

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eco-toxicity and health risk assessment of polycyclic aromatic hydrocarbons in surface sediments of Burullus Lake in egypt

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China Geology 2024年第3期7卷 460-468页

作者： Hanan e Osman Mohamed H e el-Morsy Hazem T Abd el-Hamid Department of Biology Faculty of Applied ScienceUmm Al-Qura UniversityMecca 24382Saudi Arabia Deanship of Scientific Research Umm Al-Qura UniversityMakkah 24372Saudi Arabia National Institute of Oceanography and Fisheries(NIOF) Cairo 11865Egypt Botany and Microbiology Department Faculty of ScienceAl-Azhar UniversityCairo 11651Egypt

Polycyclic aromatic hydrocarbons(PAHs)are ubiquitous environmental contaminants of growing concern due to their potential ecological and human health *** study presents a comprehensive assessment of PAHs contamination in the surface sediments of Burullus Lake,a vital and second largest delta lake in *** aim was to evaluate the eco-toxicity and potential health risks associated with the presence of these *** seven sediment samples were collected from various drains in the southern part of Burullus *** extraction method was employed to extract PAHs(16PAHs)from the sediment ***,target compounds were located using *** results showed that samples contained PAHs levels ranging from 0.038×10^(-6)to 0.459×10^(-6),which is considered heavily polluted by the european standard for PAHs ***,there was no apparent source of PAHs in the elKhashah drain or the Brinbal Canal,as HPLC found none of the *** most prevalent compound in sediment samples along the study area was *** diagnostic indices in the present study indicated that the hydrocarbons in the region originated from pyrolytic and man-made sources along the drains of Burullus *** principal component analysis(PCA)and diagnostic ratios revealed that coal combustion and pyrolytic sources were responsible for the PAHs contamination in the surface *** non-carcinogenic risk(HI),which is the product of the HQs for the adult and child populations,respectively,was *** values under 1,therefore,demonstrated that they had no carcinogenic effects on human *** and MeQs in the sediments of Burullus Lake do not have a cancer-causing impact on *** the safety of nearby wildlife,aquatic life,and people,all activities that raise petroleum hydrocarbon levels in Burullus Lake must be adequately regulated and *** to the ecological risk assessment,there is little chance that PAHs will be found

关键词： Polycyclic aromatic hydrocarbons Diagnostic indices Toxicity Delta lake sediment Burullus Lake Human health risk Aquatic ecosystem HPLC Coal combustion

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Jigsaw-Sketch: a fast and accurate algorithm for finding top-k elephant flows in high-speed networks

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Science China(Information Sciences) 2024年第4期67卷 113-130页

作者： Boyu ZHANG He HUANG Yu-e SUN Yang DU Dan WANG School of Computer Science and Technology Soochow University School of Rail Transportation Soochow University

Finding top-k elephant flows in high-speed networks is one of the most fundamental network measurement tasks. It is more challenging than per-flow size estimation since the IDs and sizes of top-k flows must be tracked simultaneously. Most existing studies only record the IDs of a small number of elephant flows to fit their estimators in the extremely limited high-speed on-chip memory. However, these solutions need too many memory accesses when a packet arrives to track the elephant flows with high accuracy, which limits their practicability. Therefore, this paper proposes Jigsaw-Sketch, a new algorithm to find the top-k elephant flows with much fewer memory accesses while achieving high memory efficiency and accuracy. In this design, we propose a novel two-stage jigsaw storage scheme, which can capture the candidate top-k flows from massive network steams efficiently, and further find the top-k elephant flows with high memory efficiency and only a few memory accesses for each packet. extensive experimental results based on real network traces show that Jigsaw-Sketch improves the packet processing throughput by at least 86%, while achieving smaller memory footprints and higher accuracy compared to the SOTA.

关键词： sketch top-$k$ network measurement elephant flow high-speed networks

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2024 Wheelchair Compendium of Physical Activities:An update of activity codes and energy expenditure values

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Journal of Sport and Health Science 2024年第1期13卷 18-23页

作者： Scott A.Conger Stephen D.Herrmann erik A.Willis Tom e.Nightingale Joseph R.Sherman Barbara e.Ainsworth Department of Kinesiology Boise State UniversityBoiseID 83725USA Kansas Center for Metabolism and Obesity Research The University of Kansas Medical CenterKansas CityKS 66160USA Center for Health Promotion and Disease Prevention University of North Carolina at Chapel HillChapel HillNC 27599USA School of Sport Exercise and Rehabilitation SciencesUniversity of BirminghamBirmingham AL B152TTUK Centre for Trauma Sciences Research University of BirminghamEdgbastonBirmingham AL B152TTUK College of Health Solutions Arizona State UniversityPhoenixAZ 85003USA School of exercise and Health Shanghai University of SportShanghai 200438China

Purpose:This paper presents an update of the 2011 Wheelchair Compendium of Physical Activities designed for wheelchair users and is referred to as the 2024 Wheelchair *** Wheelchair Compendium aims to curate existing knowledge of the energy expenditure for wheelchair physical activities(PAs).Methods:A systematic review of the published energy expenditure of PA for wheelchair users was completed between 2011 and May *** added these data to the 2011 Wheelchair Compendium data that was compiled previously in a systematic review through ***:A total of 47 studies were included,and 124 different wheelchair PA reported energy expenditure values ranging from 0.8 metabolic equivalents for wheelchair users(filing papers,light effort)to 11.8 metabolic equivalents for wheelchair users(Nordic sit skiing).Conclusion:In introducing the updated 2024 Wheelchair Compendium,we hope to bridge the resource gap and challenge the prevailing narratives that inadvertently exclude wheelchair users from physical fitness and health PAs.

关键词： Disability exercise MeT Mobility

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New insights into the role of the endoplasmic reticulum in microglia

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Neural Regeneration Research 2024年第7期19卷 1397-1398页

作者： Veronika e.Neubrand M.Rosario Sepúlveda Department of Cell Biology Faculty of SciencesUniversity of GranadaGranadaSpain

Microglial cells are the only resident immune cells in the central nervous system and constitute its frontline *** are extremely reactive against infections,trauma,or toxins,but are also responsible for mediating inflammation,taking part in the pathogenic course of many neuropathologies(Sierra et al.,2019).Cell-specific staining,ultrastructural analysis by transmission electron microscopy(TeM),or two-photonmicroscopy imaging have been relevant for the characterization of microglia as well as their cell-cell interactions。

关键词： inflammation reticulum

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Mitochondrial recruitment in myelin:an anchor for myelin dynamics and plasticity?

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Neural Regeneration Research 2024年第7期19卷 1401-1402页

作者： Jean-David M.Gothié Timothy e.Kennedy Department of Neurology and Neurosurgery Montreal Neurological InstituteMcGill UniversityMontrealQCCanada

Optimal propagation of neuronal electrical impulses depends on the insulation of axons by myelin,produced in the central nervous system by *** is an extension of the oligodendrocyte plasma membrane,which wraps around an axon to form a compact multi-layered *** is composed of a substantially higher proportion of lipids compared to other biological membranes and enriched in a small number of specialized proteins.

关键词： plasticity insulation dynamics

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