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Activation free energy of Zn(Ⅱ),Co(Ⅱ) binding to metallo-β-lactamase ImiS

Chinese Chemical Letters 2014年第10期25卷 1323-1326页

作者： Xia yang Ya-Jun Zhou Pei He Yun-Hua Guo Cong-Jun Liu ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

In an effort to understand the recombination of a B2 metallo-β-lactamase（MβL）,the binding of metals to apo-ImiS was studied by isothermal titration calorimetry and fluorescence *** binding of Zn（Ⅱ）,Co（Ⅱ） to apo-lmiS resulted in activation free energies △G_≠~θ values of 93.719 and 92.948 kJ mol^（-1）,respectively,and increasing of fluorescence intensity at maxima emission of 340 nm.

关键词： Antibiotic resistant bacteria Metallo-β-lactamases Metalloprotein recombinant Thermokinetic parameters

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One-step Synthesis of n-Butanol from Ethanol Condensation over Alumina-supported Metal Catalysts

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Chinese Chemical Letters 2004年第12期15卷 1497-1500页

作者： ke wu yang Xuan Zhen JIANG Wei Chao ZHANGD Department of Chemistry, Zhejiang University, HangZhou 310027 Department of Chemistry Zhejiang University Hangzhou 310027 China

One-step synthesis of n-butanol from bimolecular condensation of ethanol was firstlyachieved over nickel supported gamma alumina catalyst. A mechanism of dehydration path for thegrowth of carbon chain by eliminating a hydroxy group from one ethanol molecule with a α-H ofother ethanol molecule rather than aldol condensation was verified.

关键词： Ethanol condensation n-butanol nickel supported on gamma alumina dehydration

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Azolylthioacetamide:a highly promising scaffold for the development of metallo-β-lactamase inhibitors

Azolylthioacetamide:a highly promising scaffold for the deve...

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中国化学会第九届全国有机化学学术会议

作者： yang Xiang ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

The use ofβ-lactam antibiotics is compromised by drug-resistant bacteria,which employ theβ-lactamase to catalyze hydrolysis ofβ-lactam ***-β-lactamases(MβLs)are zinc-dependent hydrolases,which hydrolyze nearly almost allβ-lactam ***,developing inhibitors of MβLs is urgent and *** on our recent studies about MβL inhibitors,according to the superposition principle of biological activities,we designed and

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Synthesis and activity of phosphonate derivatives as potential inhibitors of metallo-β-lactamases

Synthesis and activity of phosphonate derivatives as potenti...

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中国化学会第九届全国有机化学学术会议

作者： Ying Ge ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

Antibiotic resistance emerged as a worldwide clinical *** most dramatic achievement against bacterial resistance is the combination of classicalβ-lactamase inhibitors(clavulanic acid,tazobactam and sulbactam)andβ-la...

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PREPARATIONS OF COPPER (Ⅰ) COMPLEXES WITH NOVEL PYRAZOLYLBORATES

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Chinese Chemical Letters 1994年第4期5卷 341-342页

作者： ke wu yang Yuan QiYIN Dao Scn JIN(Lanzhou Institute of Chemical Physics, Academia Sinica, Lanzhou 730000)

Novel pyrazolylborates, HB(3,5-Me2pz)3 and HB(3(5)-Ph pz)3 were synthesized. Several copper (Ⅰ) complexes ligated with these ligands were prepared and their properties,characterization are described in this paper.

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Design and synthesis of mercaptoacetic acid thiol ester derivatives as potential inhibitors of metallo-β-lactamase L1

Design and synthesis of mercaptoacetic acid thiol ester deri...

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中国化学会第九届全国有机化学学术会议

作者： Xiao-Long Liu ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

β-Lactam antibiotics are widely used to treat a variety of serious ***,the overuse of antibiotics has resulted in a large number of bacterial strains which resist these *** common way that bacteria become resistant toβ-lactams is through the production of metallo-β-lactamases(MβLs),which cleave theβ-lactam bond and inactivate the *** most effective way to combat antibiotic resistant bacteria is to use MβL inhibitors in combination with

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Design and synthesis of novel fluorogenic substrates for the detection of metallo-β-lactamases

Design and synthesis of novel fluorogenic substrates for the...

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中国化学会第九届全国有机化学学术会议

作者： Yi-Lin Zhang ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

＜正＞Antibiotic resistance is an emerging clinic threat worldwide due to the overuse of ***,β-lactamases have been increasingly reported as the cause of therapeutic failures in *** some classicalβ-lactamase inhibitors have successfully been used in hospital treatment,there are no inhibitors of metallo-β-lactamases（MβLs）for *** MβLs exhibit the

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Design and synthesis of azolythioacetamides as inhibitors for metallo-β-lactamses

Design and synthesis of azolythioacetamides as inhibitors fo...

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中国化学会第九届全国有机化学学术会议

作者： Ya-Nan Chang ke-wu yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

The drug-resistant bacteria have been a serious threat to the clinical *** bacteria hydrolyze almost allβ-lactam antibiotics by expressing the metallo-β-lactamses(MβLs).Therefore,it is urgent to develop the inhibitors of Mβ*** previous studies reveal that azolythioacetamides are the effective inhibitors of MβL-ImiS,in which the aromatic carboxylic plays a significant role

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Evidence-based nursing applied in oral administration in psychiatry

Evidence-based nursing applied in oral administration in psy...

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中华医学会精神病学分会第九次全国学术会议

作者： wu ke-wen and yang Wen-li 山西省荣军精神康宁医院

Evidence-based nursing(EBN)as the basis for clinical nursing decision-making process,iS being used in planned care by nurses,which combines scientific research conclusion with clinical experience and the need of the patients for acquiring the best *** initiates to provide the best service for the service ***-based nursing concepts were introduced into nursing practice in our *** we enhanced the quality of nursing control of The clinical medication,in order to regulate the administration of drugs,and the results were *** report iS drawn as follows:

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Synthesis and evaluation of boronic acids as inhibitors of metallo-β-lactamase

Synthesis and evaluation of boronic acids as inhibitors of m...

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第十届全国化学生物学学术会议

作者： yang,Xiang Li-Wei,Xu ke-wu,yang key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education and College of Chemistry and Materials Science Northwest University

The facile dissemination of genes encoding β-lactamase, enzymes capable of hydrolyzing β-lactms, is the important mechanism in antibiotic resistance.[1] According to the different active site, β-lactamase were categorized into serine-β-lactamase（SβLs） which use a Ser-OH cleave the β-lactam ring（Fig.1A）, and metallo-β-lactamases（MβLs） which is zinc-dependent. MβLs are of growing concern as a cause of all antibiotic failure.[2] Therefore, developing the inhibitor of MβLs is imperative. Boronic acids transition-state inhibitor is replace the β-lactam recognition motif with a boronic acid（Fig. 1B）, and exhibited excellent inhibitory activity against SβLs.[1] Also, the mononuclear MβL catalyzed hydrolysis of β-lactam employ hydroxyl coordinative with znic（Fig.1C）, so it is possible that boronic acid as a target of MβL（Fig.1D）. Based on this mechanism, we designed, synthesized and evaluated a penicillin G homologous boronic acid derivative 1（Fig.1E）, and the percent inhibition against ImiS（single zinc MβL） was 30% at 10 μM, using imipenem as substrate.

关键词： MβLs Inhibitor Boronic acids

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