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Chinese Chemical Letters 2005年第10期16卷 1309-1312页

作者： guo qiang hu Wen Long huANG Hai WANG Medicinal College of Henan Unversity Kaifeng 475001 China Pharmaceutical University Nanjing 210009 Academy of Military Medical Sciences Beijing 100850

6/3-（4-Chlorophenyl）-s-triazolo[3, 4-b][1, 3, 4]thiadiazoles （2,a-e） and （Sa-e） were synthesized respectively by intermolecular cyclization of 5-aryl / 4-chlorophenyl-4-amino-3- mercapto-1, 2, 4-triazoles （la-e） and （4） with 4-chlorobenzoic acid / aryl acids, which were condensed with piperazine under phase transfer catalyst TBAB to yield the corresponding free bases of monopiperazine derivatives and followed to form water-soluble salts （3a-e） and （6a-e） with hydrochloric acid in good yields. The in vitro biological results showed that piperazine group conjugated with the above fused heterocycles played an important role in antibacterial activity. The structures of novel compounds were confirmed by IR, ＇H NMR, MS and elemental analysis.

关键词： s-Triazolo[3,4-b]thiadiazole piperazine water-soluble antibacterial activity.

Synthesis of Pyridyl Polyheterocyclic Oxime-ether Schiff Bases Containing s-Triazole and Oxadiazole Subunits

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Chinese Chemical Letters 2006年第7期17卷 899-902页

作者： guo qiang hu Sheng LI Wen Long huANG Institute of Pharmacy Henan Unversity Kaifeng 475001 China Pharmaceutical University Nanjing 210009

4-Amino-5-pyridin-4-yl-s-triazole-3-thiol （1） was sequentally reacted with 3-chloro-1- phenylpropan-1-one to afford 3-（4-amino-5-pyridin-4-yl-s-triazole-3-sulfanyl）-1-phenylpropan-1- one （2） followed by oximation with hydroxylamine hydrochloride and etherification with 5-aryl-[13,4]oxadiazole-2-cbloromethanes to the corresponding oxime （3） and oxime-ethers （4a-e）, respectively. The condensation of compounds 4 with salicylaldehyde gave the title compounds （5a-e）. The antibacterial activity in vitro against Gram-postive （G^＋） and Gram negative （G） bacteria was primarily evaluated.

关键词： Pyridine triazole oxadiazole oxime-ether schiff base antibacterial activity.

Synthesis and Bioactivity of Arecoline Derivatives Containing Amino-s-triazole Coupled Oxadiazole

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Chinese Chemical Letters 2006年第1期17卷 19-22页

作者： guo qiang hu Sheng LI Wen Long huANG Hai WANG Medical College of Henan Unversity Kaifeng 475001 China Pharmaceutical University Nanjing 210009 Academy of Military Medical Sciences Beijing 100850

5-（5＂-Substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-pyridin-3′-yl- [1,2,4] triazol-4-yl amines la-j were quaternarized with methyl iodide to afford the corresponding methyl pyridinium salts 2a-j. The reduction of compounds 2 with NaBH4 in methanol gave the target compounds 5-（5＂-substituted phenyl-[1＂,3＂,4＂]oxadiazol-2＂-yl methylsulfanyl）-3-（1′-methyl-1＇,2＇,5＇,6＇-tetrahydropyridin-3＇-yl）-[1,2,4]triazol-4-ylamines 3a-j. The endothelium vascular relaxing activity of the target compounds were screened.

关键词： Tetrahydropyridine triazolylamine oxadiazole muscarinic agonist vascular activity.

Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles(Ⅱ):From triazolothiadiazines to pyrazolotriazoles

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Chinese Chemical Letters 2011年第7期22卷 804-806页

作者： guo qiang hu Li Li Hou Yong Yang Lei Yi Song qiang Xie guo qiang Wang Nan Nan Duan Tie Yao Chao Xiao Yi Wen Wen Long huang Institute of Chemistry & Biology Henan University Kaifeng 475001 China China Pharmaceutical University Nanjing 210009 China

To further expand an effective modified route for the shift from an antibacterial fluoroquinolone （FQ） to an antitumor FQ, two series of title compounds based on an isostere of the FQ C3 carboxylic group with two fused heterocyclic rings, [ 1,2,4]triazolo[3,4- b][1,3,4]thiadiazine and pyrazolo[5,1-c][1,2,4]triazole, respectively, were designed and synthesized starting from the current antibacterial FQs, and their in vitro antitumor activity against L1210, CHO cell lines were evaluated via their respective IC50 values.

关键词： Fluoroquinolone Triazolothiadiazine Pyrazolotriazole Antitumor evaluation

Synthesis and antitumor and antibacterial evaluation of fluoroquinolone derivatives(Ⅲ):Mono- and bis-Schiff-bases

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Chinese Chemical Letters 2012年第5期23卷 515-517页

作者： guo qiang hu Xiao Kui Wu guo qiang Wang Nan Nan Duan Xiao Yi Wen Tie Yao Cao Yin Jun Wang Wei Song qiang Xie Wen Long huang Institute of Chemistry&Biology Henan UniversityKaifeng 475001China China Pharmaceutical University Nanjing 210009China

To further explore an efficient modified route for the shift from an antibacterial fluoroquinolone to an antitumor one,mono-Schiff bases 6a-6h related to ciprofloxacin C3 carbonylhydrazone and bis-Schiff bases 4a-4h corresponding to C3/C7 carbonylhydrazone/hydrazone attached on a skeleton of ciprofloquinolone were designed and synthesized,and their in vitro antitumor activity against CHO,HL60,L1210 cells and antibacterial activity against Staphylococcus aureus and Escherichia coli were also reported.

关键词： Fluoroquinolone Schiff base Antitumor evaluation

Synthesis and antibacterial activity of novel[1,2,4]triazolo[3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives

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Chinese Chemical Letters 2015年第1期26卷 149-151页

作者： Liu-Zhou Gao Yu-Suo Xie Tao Li Wen-Long huang guo-qiang hu Institute of Chemical Biology.Henan University Centre of Drug Discovery China Pharmaceutical University

Novel tricyclic fluoroquinolones,[1,2,4]triazolo[3,4-h][1,8]naphthyridine-8-one-7-carboxylic acid derivatives 4a-4h bearing carrying a functional Mannich-base moiety at the C-8 position,were synthesized and evaluated for their antimicrobial *** results showed that some compounds with a piperazine side chain exhibited comparable or better antibacterial activity than comparator ***,the targeted compounds also displayed a broad spectrum of activity against resistant strains including both Gram-negative and Gram-positive *** particular,compound 4h showed an MIC of 0.25 μg/mL in antibacterial assay against multiple drug-resistant Escherichia coli,which represents an about 30-fold increase of potency compared to ***,their excellent antibacterial activity against resistant strains suggests that triazole-fused fluoroquinolones warrant further optimization as novel anti-infective chemotherapies.

关键词： Triazole Tricyclic fluoroquinolone Synthesis Antibacterial activity

Synthesis and antitumor activity of water-soluble poly(aminoheterocyclic amine)s (I): N,N,N',N'-tetra[2-(4-amino-5-substituted-s-triazol-3-yl sulfanyl)ethyl] -1,4-benzyldiamine salts

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Chinese Chemical Letters 2007年第2期18卷 124-126页

作者： guo qiang hu, Song qiang Xie, Wen Long huang Institute of Pharmacy, Henan University, Kaifeng 475001, China China Pharmaceutical University, Nanjing 210009, China Institute of Pharmacy Henan University Kaifeng 475001 China China Pharmaceutical University Nanjing 210009 China

Five water-soluble poly(aminoheterocyclic amine)s containing s-triazole ring were synthesized as respective HC1 salts (5a-5e). Biological activities in L1210 (murine leukemia) and Chinese hamster ovary (CHO) cell lines were investigated via IC50 cytotoxicity determinations. The tide compounds represented moderate cytotoxicity (low IC50 values between 15 and 68μmol/L) in L1210 but high cytotoxicity (lower IC50 values: 0.25,0.018,0.014μmol/L for Sa-5e, respectively) in CHO cell lines, while the corresponding HC1 salts of the intermediates (3a-3e) without polyamine tether and starting materials amino-s-triazoles (1a-1e) showed poor or no activities against the above cell lines.

关键词： Triazole Polyamine Water-soluble Antitumor activity

Understanding the Impact of H_(2) Diffusion Energy on the Formation Efficiency of H_(2) on the Interstellar Dust Grain Surface

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Research in Astronomy and Astrophysics 2024年第9期24卷 190-198页

作者： Xiaoying guo Wasim Iqbal qiang Chang Xiao-hu Li School of Physics and Optoeletronic Engineering Shandong University of TechnologyZibo 255000China Xinjiang Astronomical Observatory Chinese Academy of SciencesUrumqi 830011China Key Laboratory of Radio Astronomy Chinese Academy of SciencesUrumqi 830011China

We use microscopic Monte Carlo simulation techniques to investigate the impact of H_(2)diffusion energy on the recombination efficiency of H_(2)on interstellar dust grain surfaces under diffuse and translucent cloud *** constructed five models representing different possible conditions encountered by adsorbed H and H_(2)on interstellar dust *** implemented adsorption sites with multiple binding energies for surface species;the Encounter-Desorption mechanism was also *** study focused on silicate surfaces in diffuse clouds and water ice surfaces in translucent *** results show that the recombination efficiency of H_(2)on dust surfaces decreases as H_(2)diffusion energy *** interesting finding of this work is that considering different binding sites for H and H_(2)gives rise to multiple steady phases,during which the recombination efficiency remains constant with a change in H_(2)diffusion energy.

关键词： astrochemistry atomic processes ISM:molecules

Mechanistic insight into Cr(Ⅵ)retention by Si-containing ferrihydrite

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Journal of Environmental Sciences 2024年第5期139卷 217-225页

作者： Ying hu qiang Xue Honghan Chen huaming guo Kenneth C.Carroll Song Wang MOE Key Laboratory of Groundwater Circulation and Environmental Evolution School of Water Resources and EnvironmentChina University of Geosciences(Beijing)Beijing 100083China Beijing Key Laboratory of Water Resources and Environmental Engineering School of Water Resources and EnvironmentChina University of GeosciencesBeijing 100083China State Key Laboratory of Biogeology and Environmental Geology China University of GeosciencesBeijing 100083China Plant&Environmental Science New Mexico State UniversityNM 88003USA Institute of Theoretical Chemistry College of ChemistryJilin UniversityChangchun 130023China

Hexavalent chromium[Cr(Ⅵ)]causes serious harm to the environment due to its high toxicity,solubility,and ***(Fh)are the main adsorbent and trapping agent of Cr(Ⅵ)in soils and aquifers,and they usually coexist with silicate(Si),forming Si-containing ferrihydrite(Si-Fh)***,the mechanism of Cr(Ⅵ)retention by Si-Fh mixtures is poorly *** this study,the behaviors and mechanisms of Cr(Ⅵ)adsorption onto Si-Fh with different Si/Fe molar ratios was *** electron microscope,Fourier transform infrared spectroscopy,X-ray diffraction,X-ray photoelectron spectroscopy,and other techniques were used to characterize Si-Fh and Cr(Ⅵ)-loading of *** results show that specific surface area of Si-Fh increases gradually with increasing Si/Fe ratios,but Cr(Ⅵ)adsorption on Si-Fh decreases with increasing Si/Fe *** is because with an increase in Si/Fe molar ratio,the point of zero charge of Si-Fh gradually decreases and electrostatic repulsion between Si-Fh and Cr(Ⅵ)***,the complexation of Cr(Ⅵ)is enhanced due to the increase in adsorbed hydroxyl(A-OH-)on Si-Fh with increasing Si/Fe molar ratio,which partly counteracts the effect of the electrostatic ***,the increase in the electrostatic repulsion has a greater impact on adsorption than the additional complexation with *** functional theory calculation further supports this observation,showing the increases in electron variation of bonding atoms and reaction energies of inner spherical complexes with the increase in Si/Fe ratio.

关键词： Hexavalent chromium Ferrihydrite Si/Fe ratio Cr(Ⅵ)Adsorption

Spontaneous Infection and Periodic Evolving of Domain in a Diffusive SIS Epidemic Model

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Acta Mathematicae Applicatae Sinica 2024年第1期40卷 164-191页

作者： qiang Wen guo-qiang Ren Bin Liu School of Mathematics and Statistics Huazhong University of Science and TechnologyWuhan430074China hubei Key Laboratory of Engineering Modeling and Scientific Computing Huazhong University of Science and TechnologyWuhan430074China

In this paper, we consider a susceptible-infective-susceptible(SIS) reaction-diffusion epidemic model with spontaneous infection and logistic source in a periodically evolving domain. Using the iterative technique,the uniform boundedness of solution is established. In addition, the spatial-temporal risk index R0(ρ) depending on the domain evolution rate ρ(t) as well as its analytical properties are discussed. The monotonicity of R0(ρ)with respect to the diffusion coefficients of the infected dI, the spontaneous infection rate η(ρ(t)y) and interval length L is investigated under appropriate conditions. Further, the existence and asymptotic behavior of periodic endemic equilibria are explored by upper and lower solution method. Finally, some numerical simulations are presented to illustrate our analytical results. Our results provide valuable information for disease control and prevention.

关键词： diffusive SIS model spontaneous infection periodically evolving domain periodic endemic equilibrium