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Synthesis and Antibacterial Activity of Novel Oxazolidinone Analogs Containing Substituted Thiazole/Fused-Bicyclic Groups

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Chemical Research in Chinese Universities 2006年第4期22卷 459-464页

作者： ZHAI Xin ZHAO yan-fang wang Jia HONG Wei HUANG Liang GONG Ping School of Pharmaceutical Engineering Shenyang Pharmaceutical University Shenyang 110016 P. R. China

Sixteen novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic（imidazo[ 1,2-b] pyridazine/ imidazo[2,1-b] thiazole） groups were designed and synthesized. A new method for the preparation of the key intermediate compound 11 was proposed. The structures of the target compounds were confirmed by ^1H NMR, IR and MS, and their in vitro antibacterial activities against staphylococcus aureus were evaluated. Among them, compound 16a displays a promising antibacterial activity comparable to that of linezolid.

关键词： Oxazolidinone analog Synthesis Antibacterial activity

A simple Pb-doping to achieve bonding evolution, VSn and resonant level shifting for regulating thermoelectric transport behavior of SnTe

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Journal of Materials Science & Technology 2023年第20期151卷 66-72页

作者： Xu-Ye Xin Jun Ma Hong-Quan Liu Yi-Jie Gu yan-fang wang Hong-Zhi Cui College of Materials Science and Engineering Shandong University of Science and TechnologyQingdao 266590China School of Mechanical-electronic and Vehicle Engineering Weifang UniversityWeifang 261061China School of Materials Science and Engineering China University of Petroleum HuadongQingdao 266580China

The intensification of energy crises and environmental pollution inspire researchers’attention to environment-friendly SnTe thermoelectric *** this work,we achieved a lower lattice thermal conductivity and optimized the power factor via the synergistic optimization of bonding characteristic,VSn,and resonant level for the SnTe system,***-introduction produces weak bonding strength,mass fluctuation,and stress distortion,which result in lower thermal *** lowest lattice thermal conductivity achieves 0.66 W m^(–1) K^(–1) at 773 *** introduced VSn relieves loss of electrical conductivity caused by Pb-introduction,and it also makes the bigger g(E)and up-shift of resonance *** VSn,enhanced g(E),and resonant level make electrical conductivity and Seebeck coefficient enhance ***,the further optimization of thermal and electronic transport performance contributes to a higher ZT value of∼0.86 at 773 K in the Sn_(0.685)Pb_(0.285)In_(0.015)Te_(0.7)Se_(0.3) *** strategy of bonding characteristic,VSn,and resonant level synergistic engineering will be widely applicable to various TE systems for achieving better thermoelectric performance.

关键词： SnTe-based material Low thermal conductivity Projected crystal orbital hamiltonian populations VSn Resonant level

Accumulation and distribution of arsenic and cadmium by tea plants

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Journal of Zhejiang University-Science B(Biomedicine & Biotechnology) 2008年第3期9卷 265-270页

作者： Yuan-zhi SHI Jian-yun RUAN Li-feng MA Wen-yan HAN fang wang Tea Research Institute Chinese Academy of Agricultural Sciences Hangzhou 310008 China

It is important to research the rules about accumulation and distribution of arsenic and cadmium by tea plants,which will give us some scientific ideas about how to control the contents of arsenic and cadmium in *** this study,by field investigation and pot trial,we found that mobility of arsenic and cadmium in tea plants was *** arsenic and cadmium absorbed were fixed in feeding roots and only small amount was transported to the above-ground *** of arsenic and cadmium,based on their concentrations of unit dry matter,in tea plants grown on un-contaminated soil was in the order:feeding roots>stems≈main roots>old leaves>young *** tea plants were grown on polluted soils simulated by adding salts of these two metals,feeding roots possibly acted as a buffer and defense,and arsenic and cadmium were transported less to the aboveground *** concentration of cadmium in soil significantly and negatively correlated with chlorophyll content,photosynthetic rate,transpiration rate and biomass production of tea plants.

关键词： Tea plant Arsenic (As) Cadmium (Cd) Absorption Accumulation

Synthesis, Characterization and Biological Activities of N-Acyl-3-（3-pyridyl）-5-aryl-pyrazoles

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Chemical Research in Chinese Universities 2013年第2期29卷 227-230页

作者： KANG yan-fang wang Dun-jia XU Ben-po WEI Xian-hong ZHENG Jing Hubei Provincial Key Laboratory of Pollutant Analysis and Reuse Technology College of Chemistry and Environmental Engineering Hubei Normal University Huangshi 435002 P. R. China

Ten novel N-acyl-3-（3-pyridyl）-5-aryl-pyrazoles were synthesized by Claisen condensation of the aryl methyl ketones with ethyl nicotinate, the cyclization with hydrazine hydrate and the N-acylation with acyl chloride in turn. The structures of all the compounds synthesized were confirmed by means of Fourier transform infrared（FTIR）, IH NMR, mass spectroscopy and elemental analysis. The biological activities of the title compounds were examined by disc diffusion method against Escherichia coil Staphylococcus aureus, Pyricularia oryzae and Rhizoctnia solani. All the N-acyl-3-（3-pyridyl）-5-aryl-pyrazoles exhibited a certain degree of antibacterial and antifungal activities. Comparatively, compounds 3c and 3d exhibited much significant antibacterial and antifungal activities than the other pyrazole derivatives.

关键词： N-Acyl-3-(3-pyridyl)-5-aryl-pyrazole fl-Diketone 1H-Pyrazole Biological activity

First-principle study of Ba isotopic fractionation during ion exchange processes

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Acta Geochimica 2022年第1期41卷 121-131页

作者： Xin-Yue Ji yan-fang wang Le-Cai Xing Jian Liu Peng-Dong wang Tian-Di Zhang Hao-Nan Zhao School of Earth Science and Engineering Hebei University of EngineeringHandan 056038China Key Laboratory of Resource Survey and Research of Hebei Province Hebei University of EngineeringHandan 056038China

The potential utilization and development of the Ba isotope tool depend on an accurateδ^(137/134)Ba determination of the *** the chemical purification,whether the adsorption process on the surface of the ionexchange resin could lead to the Ba isotopic fractionation and the degree of fractionation directly influence the accurateδ^(137/134)Ba *** the present work,first-principles calculations based on the density functional theory were used to quantify the Ba isotopic equilibrium fractionation factor between the aqueous solution and the resin in the acid leaching *** constructing and optimizing the geometric configurations of Ba-containing species,Ba(H_(2)O)_(n)^(2+),Ba(H_(2)O)_(n)Cl_(2),Ba(H_(2)O)_(n)(NO_(3))2,and the adsorbed Ba^(2+)on the surface of the resin,extracting the harmonic vibrational frequencies,we finally at 298 K obtained the fractionations,Δ^(137/134)Ba_(soln-ads)=0.07‰,Δ^(137/134)Ba_(Ba(H_(2)O)_(n)Cl_(2)-ads)=0.05‰,andΔ^(137/134)-Ba^(Ba(H_(2)O)_(n)(NO_(3))2-ads)=0.02‰.Overall,there were almost no Ba isotope fractionations during *** the Ba isotope fractionation can be magnified by the Rayleigh fractionation process in purification,the difference inδ137/134Ba between the initial and final stages did not exceed0.060‰(or 0.045‰)when leaching the standard sample with HCl or HNO_(3),which is equal to or less than the accuracy of Ba isotopic *** a common yield of89.75%,Ba isotopic fractionation induced by incomplete recovery was 0.015‰for HCl(or 0.011‰for HNO_(3)).Finally,if the influence of an incomplete recovery on theδ137/134Ba determination needs to be ignored,the recovery is suggested to be not less than 67%for HCl(or 46%for HNO_(3)).

关键词： Ion exchange Barium Equilibrium isotopic fractionation First-principles calculations Rayleigh fractionation

Ultra-highly selective recognition of nucleosides over nucleotides by rational modification of tetralactam macrocycle and its application in enzyme assay

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Chinese Chemical Letters 2024年第6期35卷 274-278页

作者： Huan Yao Jian Qin yan-fang wang Song-Meng wang Liu-Huan Yi Shi-Yao Li fangfang Du Liu-Pan yang Li-Li wang School of Pharmaceutical Science Postdoctoral Research Station of Basic MedicineHengyang Medical SchoolUniversity of South ChinaHengyang 421001China Department of Chemistry Southern University of Science and TechnologyShenzhen 518055China

Artificial macrocycle with high binding selectivity in water is often challenging but urgently needed in various research and application ***,we report a new water-soluble biomimetic tetralactam macrocycle and realize the ultra-high selectivity to nucleosides over corresponding monophosphate nucleotides by rational *** introduction of charged groups at the periphery of endofunctionalized cavity makes the selectivity(guanosine to guanosine 5-monophosphate)increase remarkably from 100 to *** on the ultra-high selectivity of biomimetic tetralactam macrocycle,the sensitive CD73 enzyme activity assay was then achieved through product-selective fluorescence indicator displacement ***,the capability of the proposed method for inhibitor screening was successfully displayed.

关键词： Rational modification Biomimetic macrocycle Ultra-high selectivity Enzyme assay

Effect of Half-dose and Standard-dose Conjugated Equine Estrogens Combined with Natural Progesterone or Dydrogesterone on Components of Metabolic Syndrome in Healthy Postmenopausal Women： A Randomized Controlled Trial

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Chinese Medical Journal 2016年第23期129卷 2773-2779页

作者： Wei Xue yan Deng yan-fang wang Ai-Jun Sun Department of Obstetrics and Gynecology Peking Union Medical College Hospital Peking Union Medical College Chinese Academy of Medical Science~ Beijing 100730 China

Background： Menopausal hormone therapy （MHT） has been proven to have beneficial effects on several components of metabolic syndrome. However, the effects vary according to different regimens, dosages, and duration of MHT. The aim of the study was to evaluate the effect of standard-dose 0.625 mg conjugated equine estrogen （CEE） and half-dose 0.3 mg CEE daily with different progestogens in a continuous sequential regimen on postmenopausal metabolic parameters in generally healthy postmenopausal women. Methods： A prospective, open-label, randomized controlled clinical trial was conducted between February 2014 and December 2015. Totally 123 Chinese postmenopausal women with climacteric symptoms were included in this study and were randomly assigned to three groups： Group A received CEE 0.3 mg/micronized progesterone （MP） 100 mg daily; Group B received CEE 0.625 mg/MP 100 mg daily; and Group C received CEE 0.625 mg/dydrogesterone 10 mg daily. Drugs were given in a continuous sequential pattern. The duration of treatment was 12 months. Clinical, anthropometrical, and metabolic variables were measured. Data were analyzed according to intention-to-treat analysis, using Student＇s t-test and analysis of variance. Results： A total of 107 participants completed the 12-month follow-up and were included in the data analysis. At 12 months of treatment, high-density lipoprotein cholesterol and apolipoprotein A significantly increased, and low-density lipoprotein cholesterol, fasting glucose, and glycosylated hemoglobin significantly decreased in Groups B and C, compared with baseline （all P 〈 0.05）. Among the three groups, only Group C showed significantly increased triglycerides compared with baseline （ 1.61 ± 0.80 mmol/L vs. 1.21 ± 0.52 mmol/L, P 0.026）. Each group showed a neutral effect on total cholesterol, lipoprotein A, apolipoprotein B, and fasting insulin levels. No cardiovascular and venous thromboembolic events occurred in the three groups. Conclusions： Among Chinese pos

关键词： Chinese Postmenopausal Women Conjugated Equine Estrogen Dydrogesterone Menopausal Hormone Therapy Micronized Progesterone

Genetically modified pigs:Emerging animal models for hereditary hearing loss

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Zoological Research 2024年第2期45卷 284-291页

作者： Xiao wang Tian-Xia Liu Ying Zhang Liang-Wei Xu Shuo-Long Yuan A-Long Cui Wei-Wei Guo yan-fang wang Shi-Ming yang Jian-Guo Zhao State Key Laboratory of Stem Cell and Reproductive Biology Institute of ZoologyChinese Academy of SciencesBeijing 100101China Savaid Medical School University of Chinese Academy of SciencesBeijing 100049China Institute for Stem Cell and Regeneration Chinese Academy of SciencesBeijing 100101China Beijing Institute for Stem Cell and Regenerative Medicine Beijing 100101China Department of Otolaryngology-Head and Neck Surgery Institute of OtolaryngologyChinese PLA General HospitalBeijing 100853China Division of Life Sciences and Medicine University of Science and Technology of ChinaHefeiAnhui 230022China State Key Laboratory of Animal Biotech Breeding Institute of Animal ScienceChinese Academy of Agricultural SciencesBeijing100193China

Hereditary hearing loss(HHL),a genetic disorder that impairs auditory function,significantly affects quality of life and incurs substantial economic losses for *** investigate the underlying causes of HHL and evaluate therapeutic outcomes,appropriate animal models are *** have been extensively used as valuable large animal models in biomedical *** this review,we highlight the advantages of pig models in terms of ear anatomy,inner ear morphology,and electrophysiological characteristics,as well as recent advancements in the development of distinct genetically modified porcine models of hearing ***,we discuss the prospects,challenges,and recommendations regarding the use pig models in HHL ***,this review provides insights and perspectives for future studies on HHL using porcine models.

关键词： Pigs Animal models Hereditary hearing loss Genetic modification Inner ear

Anti-epileptic and Neuroprotective Effects of Ultra-low Dose NADPH Oxidase Inhibitor Dextromethorphan on Kainic Acid-induced Chronic Temporal Lobe Epilepsy in Rats

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Neuroscience Bulletin 2024年第5期40卷 577-593页

作者： Jing-Jing yang Ying-Xin Liu yan-fang wang Bi-Ying Ge Ying wang Qing-Shan wang Sheng Li Jian-Jie Zhang Ling-Ling Jin Jau-Shyong Hong Sheng-Ming Yin Jie Zhao College of Basic Medical Sciences Dalian Medical UniversityDalian116044China Department of Neurology The First Affiliated Hospital of Dalian Medical UniversityDalian116011China National and Local Joint Engineering Research Center for Drug Research and Development of Neurodegenerative Diseases Dalian116044China School of Public Health Dalian Medical UniversityDalian116044China Neurobiology Laboratory National Institute of Environmental Health SciencesNational Institutes of HealthResearch Triangle ParkDurhamNC27709USA

Neuroinflammation mediated by microglia and oxidative stress play pivotal roles in the development of chronic temporal lobe epilepsy(TLE).We postulated that kainic acid(KA)-Induced status epilepticus triggers microglia-dependent inflammation,leading to neuronal damage,a lowered seizure threshold,and the emergence of spontaneous recurrent seizures(SRS).Extensive evidence from our laboratory suggests that dextromethorphan(DM),even in ultra-low doses,has anti-inflammatory and neuroprotective effects in many animal models of neurodegenerative *** results showed that administration of DM(10 ng/kg per day;subcutaneously via osmotic minipump for 4 weeks)significantly mitigated the residual effects of KA,including the frequency of SRS and seizure *** addition,DM-treated rats showed improved cognitive function and reduced hippocampal neuronal *** found suppressed microglial activation-mediated neuroinflammation and decreased expression of hippocampal gp91^(phox) and p47^(phox) proteins in KA-induced chronic TLE ***,even after discontinuation of DM treatment,ultra-low doses of DM continued to confer long-term anti-seizure and neuroprotective effects,which were attributed to the inhibition of microglial NADPH oxidase 2 as revealed by mechanistic studies.

关键词： Temporal lobe epilepsy Dextromethorphan NADPH oxidase Ultra-low dose