检索结果-南通市图书馆

boronic acid-containing diarylpyrimidine derivatives as novel HIV-1NNRTIs: Design, synthesis and biological evaluation

在线全文

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2021年第12期32卷 4053-4057页

作者： Da Feng Fenju Wei Yanying Sun Prem Prakash Sharma Tao Zhang Hao Lin Brijesh Rathi Erik De Clercq Christophe Pannecouque Dongwei Kang Peng Zhan Xinyong Liu Department of Medicinal Chemistry Key Laboratory of Chemical Biology(Ministry of Education)School of Pharmaceutical SciencesCheeloo College of MedicineShandong UniversityJi'nan 250012China Laboratory for Translational Chemistry and Drug Discovery Department of ChemistryHansraj CollegeUniversity of DelhiDelhi 110007India Rega Institute for Medical Research Laboratory of Virology and ChemotherapyK.U.LeuvenLeuven B-3000Belgium China-Belgium Collaborative Research Center for Innovative Antiviral Drugs of Shandong Province Ji'nan 250012China Suzhou Research Institute Shandong UniversitySuzhou 215123China

Drug resistance remains to be a serious problem with type Ⅰ human immunodeficiency virus(HIV-1) nonnucleoside reverse transcriptase inhibitors(NNRTIs). A series of novel boronic acid-containing diarylpyrimidine(DAPY) derivatives were designed via bioisosterism and scaffold-hopping strategies,taking advantage of the ability of a boronic acid group to form multiple hydrogen bonds. The target compounds were synthesized and evaluated for their anti-HIV activities and cytotoxicity in MT-4 *** 10 j yielded the most potent activity and turned out to be a single-digit nanomolar inhibitor towards the HIV-1 ⅢB [wild-type(WT) strain], L100 I and K103 N strains, with 50% effective concentration(EC_(50)) values of 7.19–9.85 nmol/L. Moreover, 10 j inhibited the double-mutant strain RES056 with an EC_(50) value of 77.9 nmol/L, which was 3.3-more potent than that of EFV(EC_(50)= 260 nmol/L) and comparable to that of ETR(EC_(50)= 32.2 nmol/L). 10j acted like classical NNRTIs with high affinity for WT HIV-1 reverse transcriptase(RT) with 50% inhibition concentration(IC_(50)) value of 0.1837 μmol/L. Furthermore,molecular dynamics simulation indicated that 10 j was proposed as a promising molecule for fighting against HIV-1 infection through inhibiting RT activity. Overall, the results demonstrated that 10 j could serve as a lead molecule for further modification to address virus-drug resistance.

关键词： HIV-1 NNRTIs NNIBP DAPY boronic acid Molecular dynamics simulation

boronic acid-rich dendrimer for efficient intracellular peptide delivery

在线全文

学校读者我要写书评

暂无评论

Science China Materials 2020年第4期63卷 620-628页

作者： Jia Lv Chongyi Liu Kexin Lv Hui Wang Yiyun Cheng South China Advanced Institute for Soft Matter Science and Technology School of Molecular Science and EngineeringSouth China University of TechnologyGuangzhou 510640China Shanghai Key Laboratory of Regulatory Biology School of Life SciencesEast China Normal UniversityShanghai 200241China

Interests in intracellular peptide delivery have continued to grow,significantly fueled by the importance of peptides and their mimetics in modern cell biology and pharmaceutical ***,efficient intracellular delivery of membrane-impermeable peptides of different polarities remains a challenging *** this study,we develop a general and robust strategy for intracellular peptide delivery by using a boronic acid-rich *** designed material is capable of transporting peptides with different polarities and charge properties into the cytosol of various cell lines without inducing additional *** transduction efficacy and proteolytic stability of cargo peptides delivered by the boronic acid-rich dendrimer are much superior to peptides conjugated with cell penetrant peptides such as *** addition,the bioactivities of pro-apoptotic peptides are maintained after intracellular *** study provides a versatile and robust platform for the intracellular delivery of membrane-impermeable peptides.

关键词： intracellular peptide delivery dendrimer boronic acid

A High Sensitive LC-MS/MS Method for the Simultaneous Determination of Potential Genotoxic Impurities Carboxy Phenyl boronic acid and Methyl Phenyl boronic acid in Lumacaftor

在线全文

学校读者我要写书评

暂无评论

American Journal of Analytical Chemistry 2021年第3期12卷 74-86页

作者： Kartheek Srinivas Chidella Vijaya Bharathi Dasari A. Jayashree Center for Chemical Sciences and Technology Institute of Science and Technology Jawaharlal Nehru Technological University Hyderabad Hyderabad Telangana Aurobindo Pharma Laboratory Research Center II Hyderabad Telangana

A simple, rapid, and highly sensitive LC-MS/MS method has been developed for the simultaneous and trace level quantification of underivatized boronic acids in lumacaftor active pharmaceutical ingredient. Chromatographic separation of boronic acids and lumacaftor achieved using Agilent Poroshell HPH C18 150 × 4.6 mm 2.7 μ column with 0.1% ammonia in water as mobile phase A and 100% acetonitrile as mobile phase B at a flow rate of 0.25 ml/min. Gradient elution was used with a total method run time of 14 minutes. Boronic acids were successfully ionized and quantified without derivatization using electrospray ionization in negative mode using tandem quadrupole mass spectrometry in multiple reactions monitoring mode. Method validation was performed as per ICH guidelines with good linearity over the concentration range of 0.05 ppm to 5 ppm of Lumacaftor test concentration for both the boronic acids with a correlation coefficient of >0.99. Recoveries were found good at different concentration levels and within the range of 80% - 120%. The developed method can be successfully used for the routine quantification of boronic acids at a concentration level of 20 ng/ml (1 ppm with respect to 20 mg/ml lumacaftor).

关键词： boronic acid Genotoxic LC-MS/MS Lumacaftor

A Long-Wavelength Fluorescent Probe for Saccharides Based on boronic-acid Receptor

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Chinese Journal of Chemistry 2013年第8期31卷 1095-1101页

作者： Hongyan Bai Qian Sun Haiyu Tian Junhong Qian Lingyi Zhang Weibing Zhang Shanghai Key Laboratory of Scene Evidence Center of Material Evidence Identification Shanghai Public Security Bureau Shanghai 200083 China Shanghai Key Laboratory of Functional Materials Chemistry School of Chemistry and Molecular Engineering East China University of Science and Technology Shanghai 200237 China Email: Junhong Qian (junhongqian@***) Weibing Zhang (weibingzhang@***)[*]Shanghai Key Laboratory of Scene Evidence Center of Material Evidence Identification Shanghai Public Security Bureau Shanghai 200083 China Tel.: 0086-021-64253068 Fax: 0086-021-64233068

A single boronic acid-based fluorescent probe （compound CSP） for saccharides was designed and synthesized. The probe, with an a,fl-unsaturated ketone conjugated into the coumarin fluorophore, was synthesized by 4 steps from the commercial material 4-diethylamino salicylaldehyde. The electron push-pull effect is enhanced with the N,N-diethyl amino as the electron donor and the carbonyl as the electron acceptor. Both the absorption （463 nm） and emission （616 nm） maxima of CSP are in the visible wavelength region with a Stokes shift of about 150 nm, which ensures CSP a potential probe for biological application. Under near physiological conditions, significant fluores- cence enhancement of CSP was observed upon the addition of some saccharides, namely, D-sorbitol, D-fructose, D-glucose, D-mannose and D-galactose. The probe showed relatively high sensitivity towards D-fructose and D-sorbitol, and their detection limits were 0.05 mmol/L and 0.1 mmol/L, respectively.

关键词： saccharides coumarin boronic acid fluorescent probe

Design and synthesis of boronic acid derivatives as inhibitors of metallo-β-lactamases

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Design and synthesis of boronic acid derivatives as inhibito...

Cu2O-Mediated Room Temperature Cyanation of Aryl boronic acids/Esters and TMSCN

第十届全国化学生物学学术会议

作者： Liwei Xu Kewu Yang Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education College of Chemistry and Materials ScienceNorthwest University

β-Lactamases catalyzed hydrolysis of β-lactam antibiotics, such as penicillins, cephalosporins, and carbapenems, and are the most widespread bacterial resistance mechanism to these drugs[1]. However, the overuse of these antibiotics has resulted in a large number of bacteria with metallo-β-lactamases（MβLs） becoming resistant to most commonly-used antibiotics[2]. MβLs are Zn（II）-dependent and hydrolyze nearly all known β-lactam-containing antibiotics[3]. To date, there are no known clinical inhibitors of the MβLs to be reported. Therefore, synthesis and developing inhibitors of MβLs are needed urgently. In this paper, we reported the synthesis of boronic acid derivatives as potential inhibitors of MβLs（Scheme 1）.

关键词： Metallo-β-lactamases Inhibitor boronic acid

来源： cnki会议评论

在线全文

cnki会议

学校读者我要写书评

暂无评论

Chinese Journal of Chemistry 2013年第1期31卷 27-30页

作者： Yong Ye Yanhua Wang Pengtang Liu Fushe Han Changchun Institute of Applied Chemistry Chinese Academy of Sciences 5625 Renmin Street Changchun Jilin 130022 China State Key Laboratory of Fine Chemicals Dalian University of Technology Dalian Liaoning 116024 China Changchun University of Science and Technology Changchun Jilin 130022 China

A method for the efficient and reliable synthesis of aryl nitriles via the Cu20-catalyed cross-coupling of aryl boronic acids or esters and TMSCN is presented. A broad range of substrates decorated by electron-rich and defi- cient, sterically very congested, and labile functionalities were tolerated. Moreover, the reaction can proceed under mild conditions at room temperature. These advantages paired with the use of cheap, readily available, and halo- gen-free Cu20 as catalysts make the protocol an appealing option for aryl cyanations.

关键词： copper boronic acid boronic ester cyanation aryl nitrile

A photoactivatable and phenylboronic acid-functionalized nanoassembly for combating multidrug-resistant gram-negative bacteria and their biofilms

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Burns & Trauma 2023年第1期11卷 765-791页

作者： Xiaoqing Zhou Lanlan Dong Baohua Zhao Guangyun Hu Can Huang Tengfei Liu Yifei Lu Mengxue Zheng Yanlan Yu Zengjun Yang Shaowen Cheng Yan Xiong Gaoxing Luo Wei Qian Rui Yin Department of Dermatology Southwest HospitalArmy Medical University(Third Military Medical University)No.29 Gaotanyan RoadShapingba DistrictChongqing 400038China Institute of Burn Research State Key Laboratory of TraumaBurn and Combined InjuryKey Laboratory of Disease Proteomics of ChongqingSouthwest HospitalArmy Medical University(Third Military Medical University)No.29 Gaotanyan RoadShapingba DistrictChongqing 400038China Department of Burn and Plastic Sugery No.906 Hospital of Joint Logistic Support Force of PLANo.377 Zhongshan East RoadYinzhou DistrictNingbo 315100China Department of Wound Repair the First Affiliated Hospital of Hainan Medical UniversityNo.31 Longhua RoadHaikou 570102China Department of Orthopaedics Daping HospitalArmy Medical University(Third Military Medical University)No.10 Changjiang Branch RoadYuzhong DistrictChongqing 400042China

Background:Multidrug-resistant(MDR)gram-negative bacteria-related infectious diseases have caused an increase in the public health burden and ***,the formation of biofilms makes these bacteria difficult to ***,developing novel interventions to combat MDR gram-negative bacteria and their biofilms-related infections are urgently *** purpose of this study was to develop a multifunctional nanoassembly(IRNB)based on IR-780 and N,N-di-sec-butyl-N,N-dinitroso-1,4-phenylenediamine(BNN6)for synergistic effect on the infected wounds and subcutaneous abscesses caused by gram-negative ***:The characterization and bacteria-targeting ability of IRNB were *** bac-tericidal efficacy of IRNB against gram-negative bacteria and their biofilms was demonstrated by crystal violet staining assay,plate counting method and live/dead staining in *** antibacterial efficiency of IRNB was examined on a subcutaneous abscess and cutaneous infected wound model in vivo.A cell counting kit-8 assay,Calcein/PI cytotoxicity assay,hemolysis assay and intravenous injection assay were performed to detect the biocompatibility of IRNB in vitro and in ***:Herein,we successfully developed a multifunctional nanoassembly IRNB based on IR-780 and BNN6 for synergistic photothermal therapy(PTT),photodynamic therapy(PDT)and nitric oxide(NO)effect triggered by an 808 nm *** nanoassembly could accumulate specifically at the infected sites of MDR gram-negative bacteria and their biofilms via the covalent coupling *** irradiation with an 808 nm laser,IRNB was activated and produced both reactive oxygen species(ROS)and *** local hyperthermia could induce NO generation,which further reacted with ROS to generate ONOO−,leading to the enhancement of bactericidal ***,NO and ONOO−could disrupt the cell membrane,which converts bacteria to an extremely susceptible state and further enhances the phototherma

关键词： Photothermal therapy Photodynamic therapy Nitric oxide Synergistic boronic acid Multidrug-resistant gram-negative bacteria

A BINOL Based Fluorescence Sensor for Distinction of D-Glucose

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Chinese Journal of Chemistry 2015年第1期33卷 101-106页

作者： Bangyu Xu Jiting Hou Kun Li Zhengwei Lu Xiaoqi Yu Key Laboratory of Green Chemistry and Technology(Ministry of Education) College of ChemistrySichuan UniversityChengduSichuan 610064China

A saccharide fluorescent receptor based on 1,1'-binaphthol was *** boronic acids groups are di-rectly attached to the 3,3'-positions of BINOL which acted as probes to *** methyl protected receptor R1 showed better response to D-fructose compared to other saccharides in the fluorescence quenching *** improve the selectivity of D-glucose,the triethylene glycol protected receptor R2 was *** R2 has a better water-solubility than R1 that can be applied in completely aqueous *** receptor R2,D-glucose has a different response to other saccharides that can be useful for the distinction of D-glucose.

关键词： 1,1'-binaphthol boronic acid D-glucose distinction

Quantitative detection of citrate for early stage diagnosing of prostate cancer:Discriminating normal to cancer in prostate tissues

在线全文

维普期刊数据库

学校读者我要写书评

暂无评论

Chinese Chemical Letters 2024年第2期35卷 501-506页

作者： Selvaraj Muthusamy Kanagaraj Rajalakshmi Palanisamy Kannan Yun-Sik Nam Dongwei Zhu Yeonggil Seo Jong-Won Song Dong Nyoung Heo Il Keun Kwon Yuanguo Xu School of Chemistry and Chemical Engineering Jiangsu UniversityZhenjiang 212013China College of Biological Chemical Sciences and EngineeringJiaxing UniversityJiaxing 314001China Advanced Analysis Center Korea Institute of Science & TechnologySeongbuk-guSeoul02792Republic of Korea School of Medicine Jiangsu UniversityZhenjiang 212013China Department of Chemistry Education Daegu UniversityGyeongsan-siGyeongsangbuk-do 38453Republic of Korea Department of Dental Materials School of DentistryKyung Hee UniversitySeoulRepublic of Korea

Prostate cancer(PC)biomarker-citrate detection is clinically important to diagnose PC in early *** iodide(Q)conjugated indole-phenylboronic acid(IB)was designed as a red-emissive QIB probe for the detection of citrate through Lewis acid-base reaction and intramolecular charge transfer(ICT)sensing *** acid acts as Lewis acid as well as citrate(Lewis base)recognition *** probe reacted with citrate,showing enhanced red *** the probe has excellent water solubility and great biocompatibility,practical application in biological systems is *** was monitored precisely in the mitochondria organelle(in vitro)of living cells with a positive charge on ***,endogenous(in situ)citrate was detected quantitatively to discriminate non-cancerous and PC mice,observed strong and lower(negligible)emission intensity on non-cancerous and cancerous prostate tissues,***,the concentration of citrate is higher in healthy prostate compared with PC ***,the analysis of sliced prostate tissues can give PC-related information for clinical diagnosis to prevent and treat PC in the initial ***,we believe that the present probe is a promising biochemical reagent in diagnosing PC.

关键词： Prostate cancer Biomarker-citrate boronic acid Lewis acid/base-ICT Red-emissive Mitochondria targeting Prostate tissue