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Synthesis,pharmacokinetics and in vivo antifungal activity of the novel water-soluble prodrugs of itraconazole analogue YL-24

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Chinese Chemical Letters 2013年第4期24卷 321-324页

作者： Yu Liu xu-feng cao Xin Liu Yong-Bing cao Wen-Jing Chu Yu-She Yang State Key Laboratory of Drug Research Shanghai Institute of Materia MedicaChinese Academy of Sciences School of Pharmacy Second Military Medical University State Key Laboratory of Drug Research Shanghai Institute of Materia MedicoChinese Academy of Sciences

To improve the aqueous solubility of an itraconazole analogue, compound 1 （YL-24）, a series of novel prodrugs were synthesized. Among these prodrugs, the phosphate disodium salt compound 7 exhibited excellent aqueous solubility （9.8 mg/mL） at near-neutral pH and sufficient stability in buffer solutions, along with favorable pharmacokinetic profiles. In particular, compounds 1 and 7 provided moderate survival efficacy in murine systemic Candida albicans SC5314 infection model, but their efficacy was weaker than that of fluconazole.

关键词： SynthesisAntifungalWater-soluble prodrugsltraconazole analogue

Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents

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Chinese Chemical Letters 2016年第5期27卷 703-706页

作者： Yuan-Yuan xu An-Ran Qian xu-feng cao Chen-Yu Ling Yong-Bing cao Rui-Lian Wang Yi-Su Li Yu-She Yang State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China School of Pharmacy Second Military Medical University Shanghai 200433 China Drug Discovery and Design Center State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China

A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds were evaluated, The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.

关键词： Synthesis Triazole γ-Lactam Antifungal activity

Failure rate analysis and maintenance plan optimization method for civil aircraft parts based on data fusion

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Chinese Journal of Aeronautics 2025年第1期38卷 306-324页

作者： Kang cao Yongjie ZHANG Jianfei feng School of Civil Aviation Northwestern Polytechnical UniversityXi’an 710072China Shanghai Aircraft Design and Research Institute Shanghai 201210China

In the face of data scarcity in the optimization of maintenance strategies for civil aircraft,traditional failure data-driven methods are encountering challenges owing to the increasing reliability of aircraft *** study addresses this issue by presenting a novel combined data fusion algorithm,which serves to enhance the accuracy and reliability of failure rate analysis for a specific aircraft model by integrating historical failure data from similar models as supplementary *** a comprehensive analysis of two different maintenance projects,this study illustrates the application process of the *** upon the analysis results,this paper introduces the innovative equal integral value method as a replacement for the conventional equal interval method in the context of maintenance schedule *** Monte Carlo simulation example validates that the equivalent essential value method surpasses the traditional method by over 20%in terms of inspection efficiency *** discovery indicates that the equal critical value method not only upholds maintenance efficiency but also substantially decreases workload and maintenance *** findings of this study open up novel perspectives for airlines grappling with data scarcity,offer fresh strategies for the optimization of aviation maintenance practices,and chart a new course toward achieving more efficient and cost-effective maintenance schedule optimization through refined data analysis.

关键词： Small sample data Data fusion Failure rate Maintenance planning Aircraft parts

Mitophagy in acute central nervous system injuries:regulatory mechanisms and therapeutic potentials

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Neural Regeneration Research 2025年第9期20卷 2437-2453页

作者： Siyi xu Junqiu Jia Rui Mao Xiang cao Yun xu Department of Neurology Nanjing Drum Tower HospitalClinical College of Jiangsu UniversityNanjingJiangsu ProvinceChina Department of Neurology Nanjing Drum Tower HospitalChinese Academy of Medical Science&Peking Union Medical CollegeNanjingJiangsu ProvinceChina Department of Neurology Nanjing Drum Tower HospitalAffiliated Hospital of Medical SchoolNanjing UniversityNanjingJiangsu ProvinceChina State Key Laboratory of Pharmaceutical Biotechnology and Institute of Translational Medicine for Brain Critical Diseases Nanjing UniversityNanjingJiangsu ProvinceChina Jiangsu Key Laboratory for Molecular Medicine Medical School of Nanjing UniversityNanjingJiangsu ProvinceChina Nanjing Neurology Medical Center NanjingJiangsu ProvinceChina

Acute central nervous system injuries,including ischemic stro ke,intracerebral hemorrhage,subarachnoid hemorrhage,traumatic brain injury,and spinal co rd injury,are a major global health *** optimal therapies and improving the long-term neurological functions of patients with acute central nervous system injuries are urgent *** are susceptible to damage after acute central nervous system injury,and this leads to the release of toxic levels of reactive oxygen species,which induce cell ***,a selective form of autophagy,is crucial in eliminating redundant or damaged mitochondria during these *** evidence has highlighted the significant role of mitophagy in acute central nervous system *** this review,we provide a comprehensive overview of the process,classification,and related mechanisms of *** also highlight the recent developments in research into the role of mitophagy in various acute central nervous system injuries and drug therapies that regulate *** the final section of this review,we emphasize the potential for treating these disorders by focusing on mitophagy and suggest future research paths in this area.

关键词： autophagy intracerebral hemorrhage ischemic stroke mitochondria mitochondrial biogenesis mitochondrial quality control mitophagy spinal cord injury subarachnoid hemorrhage traumatic brain injury

Constructing Pr-doped CoOOH catalytic sites for efficient electrooxidation of 5-hydroxymethylfurfural

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Journal of Energy Chemistry 2025年第1期100卷 234-244页

作者： Botao Fan Hao Zhang Bang Gu feng Qiu Qiue cao Wenhao Fang School of Chemical Science and Technology Yunnan UniversityKunming 650091YunnanChina National Center for International Research on Photoelectric and Energy Materials School of Materials and EnergyYunnan UniversityKunming 650091YunnanChina

Electrocatalytic conversion of renewable biomass is emerging as a promising route for sustainable chemical production;hence it urgently calls for developing efficient electrocatalysts with low potentials and high current ***,a Pr-doped Co(OH)_(2)hexagonal sheet(Pr/Co=1/9,in mole)is synthesized by electrodeposition as highly performant catalyst for 5-hydroxymethylfurfural(HMF)oxidation reaction(HMFOR)to produce 2,5-furandicarboxylic acid(FDCA).This novel and low-cost catalyst possesses a rather low onset potential of 1.05 V(***)and requires only 1.10 V(***)to reach a current density of 10 mA cm^(-2)for HMFOR,significantly outperforming Co(OH)_(2)benchmark(i.e.,210 mV higher to reach10 m A cm^(-2)).The origin of Pr promotion effect as well as the evolution of CoOOH catalytic sites and HMFOR process has been deeply elucidated by physical characterizations,kinetic experiments,in situ electrochemical techniques,and theoretical *** unique Pr-ameliorated CoOOH active centers enable 100%conversion of HMF,99.6%selectivity of FDCA,and 99.7%Faraday efficiency,with a superior cycling durability toward *** can be one of the most outstanding results for Co-based HMFOR catalysts to date in the *** this work can help open up new horizons for constructing novel and efficient Co-based electrocatalysts by the utilization of lanthanide elements.

关键词： Biomass conversion Electrocatalysis 2,5-Furandicarboxylic acid Doped Co catalyst Co3+active sites Charge transfer rate

DecMamba:Mamba Utilizing Series Decomposition for Multivariate Time Series Forecasting

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Computers, Materials & Continua 2025年第1期82卷 1049-1068页

作者： Jianxin feng Jianhao Zhang Ge cao Zhiguo Liu Yuanming Ding Communication and Network Key Laboratory Dalian UniversityDalian116622China

Multivariate time series forecasting iswidely used in traffic planning,weather forecasting,and energy *** decomposition algorithms can help models better understand the underlying patterns of the original series to improve the forecasting accuracy of multivariate time ***,the decomposition kernel of previous decomposition-based models is fixed,and these models have not considered the differences in frequency fluctuations between *** problems make it difficult to analyze the intricate temporal variations of real-world time *** this paper,we propose a series decomposition-based Mamba model,DecMamba,to obtain the intricate temporal dependencies and the dependencies among different variables of multivariate time series.A variable-level adaptive kernel combination search module is designed to interact with information on different trends and periods between *** backbone structures are proposed to emphasize the differences in frequency fluctuations of seasonal and trend *** with superior performance is used instead of a Transformer in backbone structures to capture the dependencies among different variables.A new embedding block is designed to capture the temporal features better,especially for the high-frequency seasonal component whose semantic information is difficult to acquire.A gating mechanism is introduced to the decoder in the seasonal backbone to improve the prediction accuracy.A comparison with ten state-of-the-art models on seven real-world datasets demonstrates that DecMamba can better model the temporal dependencies and the dependencies among different variables,guaranteeing better prediction performance for multivariate time series.

关键词： Data prediction time series Mamba series decomposition

Predicting the efficiency of arsenic immobilization in soils by biochar using machine learning

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Journal of Environmental Sciences 2025年第1期147卷 259-267页

作者： Jin-Man cao Yu-Qian Liu Yan-Qing Liu Shu-Dan xue Hai-Hong Xiong Chong-Lin xu Qi xu Gui-Lan Duan State Key Lab of Urban and Regional Ecology Research Center for Eco-Environmental SciencesChinese Academy of SciencesBeijing 100085China Henan Institute of Advanced Technology Zhengzhou UniversityZhengzhou 450052China University of Chinese Academy of Sciences Beijing 100049China

Arsenic(As)pollution in soils is a pervasive environmental *** immobilization offers a promising solution for addressing soil As *** efficiency of biochar in immobilizing As in soils primarily hinges on the characteristics of both the soil and the ***,the influence of a specific property on As immobilization varies among different studies,and the development and application of arsenic passivation materials based on biochar often rely on empirical *** enhance immobilization efficiency and reduce labor and time costs,a machine learning(ML)model was employed to predict As immobilization efficiency before biochar *** this study,we collected a dataset comprising 182 data points on As immobilization efficiency from 17 publications to construct three ML *** results demonstrated that the random forest(RF)model outperformed gradient boost regression tree and support vector regression models in predictive *** importance analysis and partial dependence plots based on the RF model were conducted to identify the most crucial factors influencing As *** findings highlighted the significant roles of biochar application time and biochar pH in As immobilization efficiency in ***,the study revealed that Fe-modified biochar exhibited a substantial improvement in As *** insights can facilitate targeted biochar property design and optimization of biochar application conditions to enhance As immobilization efficiency.

关键词： Biochar Arsenic immobilization Soil Machine learning

Failure mechanisms of AlGaN/GaN HEMTs irradiated by high-energy heavy ions with and without bias

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Nuclear Science and Techniques 2025年第1期36卷 49-58页

作者： Pei-Pei Hu Li-Jun xu Sheng-Xia Zhang Peng-Fei Zhai Ling Lv Xiao-Yu Yan Zong-Zhen Li Yan-Rong cao xue-feng Zheng Jian Zeng Yuan He Jie Liu Institute of Modern Physics Chinese Academy of Sciences(CAS)Lanzhou 730000China Key Laboratory of Wide Band‑gap Semiconductor Materials Ministry of EducationXidian UniversityXi’an 710071China University of Chinese Academy of Sciences(UCAS) Beijing 100049China

Gallium nitride(GaN)-based devices have significant potential for space ***,the mechanisms of radiation damage to the device,particularly from strong ionizing radiation,remains *** study investigates the effects of radiation on p-gate AlGaN/GaN high-electron-mobility transistors(HEMTs).Under a high voltage,the HEMT leakage current increased sharply and was accompanied by a rapid increase in power density that caused"thermal burnout"of the *** addition,a burnout signature appeared on the surface of the burned devices,proving that a single-event burnout effect ***,degradation,including an increase in the on-resistance and a decrease in the breakdown voltage,was observed in devices irradiated with high-energy heavy ions and without *** latent tracks induced by heavy ions penetrated the heterojunction interface and extended into the GaN ***,a new type of N_(2)bubble defect was discovered inside the tracks using Fresnel *** accumulation of N_(2)bubbles in the heterojunction and buffer layers is more likely to cause leakage and *** study indicates that electrical stress accelerates the failure rate and that improving heat dissipation is an effective reinforcement method for GaN-based devices.

关键词： GaN HEMTs Heavy ions Single-event burnout Latent tracks Degradation

Xiangshao Granules Ameliorate Post-stroke Depression by Inhibiting Activation of Microglia and IDO1 Expression in Hippocampus and Prefrontal Cortex

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Chinese Journal of Integrative Medicine 2025年第1期31卷 28-38页

作者： LI Cheng-gang xu Lu-shan SUN Liang xu Yu-hao cao Xiang ZHAO Chen-chen XIA Sheng-nan ZHANG Qing-xiu xu Yun Department of Neurology Nanjing Drum Tower HospitalAffiliated Hospital of Medical SchoolNanjing UniversityNanjing210008China State Key Laboratory of Pharmaceutical Biotechnology and Institute of Translational Medicine for Brain Critical Diseases Nanjing UniversityNanjing210008China Jiangsu Key Laboratory for Molecular Medicine Medical School of Nanjing UniversityNanjing210008China Nanjing Neurology Medical Center Nanjing210008China

Objective To investigate the therapeutic effect of Xiangshao Granules(XSG)on post-stroke depression(PSD)and explore the underlying *** Forty-three C57BL/6J mice were divided into 3 groups:sham(n=15),PSD+vehicle(n=14),and PSD+XSG(n=14)groups according to a random number *** PSD models were constructed using chronic unpredictable mild stress(CUMS)after middle cerebral artery occlusion(Mcao).The sham group only experienced the same surgical operation,but without MACO and CUMS *** XSG group received XSG(60 mg/kg per day)by gavage for 4 *** mice in the sham and vehicle groups were given the same volume of 0.9%saline at the same *** body weight and behavior tests including open field test,sucrose preference test,tail suspension test,and elevated plus-maze test,were used to validate the PSD mouse ***-time fluorescence quantitative polymerase chain reaction(RT-qPCR),enzyme-linked immunosorbent assay(ELISA),and immunofluorescence staining were used to evaluate the anti-inflammatory effects of *** potential molecular mechanisms were explored and verified through network pharmacology analysis,Nissl staining,Western blot,ELISA,and RT-qPCR,*** The body weight and behavior tests showed that Mcao combined with CUMS successfully established the PSD *** alleviated neuronal damage,reduced the expressions of pro-apoptotic proteins Caspase-3 and B-cell lymphoma-2(BCL-2)-associated X(BAX),and increased the expression of anti-apoptotic protein BCL-2 in PSD mice(P<0.05 or P<0.01).XSG inhibited microglial activation and the expressions of pro-inflammatory cytokines including tumor necrosis factor-α,interleukin(IL)-1β,and IL-6 via the toll-like receptor 4/nuclear factor kappa-B signaling pathway in PSD mice(P<0.05 or P<0.01).Furthermore,XSG decreased the expression of indoleamine 2,3-dioxygenase1(IDO1)and increased the concentration of 5-hydroxytryptamine in PSD mice(P<0.05 or P<0.01).Conclusion XSG could reverse

关键词： post-stroke depression Xiangshao Granules indoleamine 2,3-dioxygenase 1 Chinese medicine