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81.
报道一条适合工业化生产合成厄他培南侧链盐酸盐的方法.采用低价易得的4R-羟基-L-脯氨酸为原料,经过氨基保护、羟基活化、硫代,水解等步骤合成了标题化合物.其中除氨基保护步骤外,其余步骤采取"一锅法"合成.收率达到70.4%. 相似文献
82.
The working performance of agricultural machinery is largely determined by the walking performance of the wheel when driving in complex unstructured soil. However, the driving performance of existing wheels is not satisfactory for paddy field with muddy soil. The purpose of the current study is therefore to propose a novel rigid wheel for agricultural machinery which is applicable to paddy field with muddy soil. Firstly, a novel arc edge shaped wheel was designed based on the principles of mechanics on the ground. Then the driving performance of this arc edge shaped wheel was evaluated using FE modeling of interaction between rigid wheel and soil. Finally, the structure originally designed arc edge shaped wheel was improved according to FE modeling results, and this improved design was further evaluated by both FE simulation and prototype experiments. Both FE modeling and experimental results indicate that the improved arc edge shaped wheel proposed in this study has a good driving performance with regarding to wheel sinkage and soil reaction force. The proposed arc edge shaped wheel could be used as an effective component of rice harvester for paddy field with muddy soil. 相似文献
83.
固相萃取液相色谱-质谱/质谱联用测定河水中大环内酯类抗生素 总被引:19,自引:4,他引:19
应用固相萃取(SPE)及LC—MS/MS技术,建立了水中痕量大环内酯类抗生素即红霉素、脱水红霉素、罗红霉素的分析方法,优化了固相萃取、液相色谱-质谱/质谱等相关条件。水样经HLB固相萃取柱富集净化,以多反应检测方式(MRM)对待测物进行定性和定量分析。3种抗生素在10-2000ng/L范围内具有良好的线性。其定量下限为5ng/L(S/N〉10)。加标纯水和实际水样的回收率在71%-111%之间,相对标准偏差(RSD)在3.7%-8.6%之间。该方法灵敏度高、选择性好、准确度高,适合实际水样中痕量大环内酯类药物的检测。使用该方法测得珠江广州河段某水样中红霉素、脱水红霉素和罗红霉素质量浓度分别为164、291和134ng/L。 相似文献
84.
85.
铂纳米颗粒在汽车行业中被广泛用作汽车尾气催化剂。随着铂纳米颗粒在工业生产中的广泛应用,它在环境中广泛分布并可能从植物累积进入食物链中。因此,建立一种在农产品中的定量分析方法是至关重要的。以酶消解的前处理方法结合单颗粒-电感耦合等离子体质谱法(Single particle ICP-MS,SP-ICP-MS)测定农产品中纳米铂颗粒(PtNPs)粒径分布及颗粒数量浓度。通过优化前处理提取条件,当Macerozyme R-10酶为10 mg、柠檬酸缓冲溶液浓度为5 mmol/L、提取时间36 h时,农产品中PtNPs提取效果较高。PtNPs粒径检出限为20 nm,颗粒浓度检出限为5×105 particle/L,铂颗粒浓度回收率在(81±3)%~(91±4)%,加标后平均粒径(41±3)~(47±2)nm,与50 nm PtNPs标准溶液粒径接近。方法操作简单、检出限低、准确度高,适用于农产品中PtNPs定量分析,为客观评价农产品铂纳米毒性效应提供可靠的分析技术。 相似文献
86.
Dr. Andreas A. Bastian Dr. Maria Bastian Dr. Manuel Jäger Mark Loznik Dr. Eliza M. Warszawik Xintong Yang Dr. Nabil Tahiri Dr. Peter Fodran Prof. Dr. Martin D. Witte Anne Thoma Dr. Jens Köhler Prof. Dr. Adriaan J. Minnaard Prof. Dr. Andreas Herrmann 《Chemistry (Weinheim an der Bergstrasse, Germany)》2022,28(36):e202200883
The continuous emergence of antimicrobial resistance is causing a threat to patients infected by multidrug-resistant pathogens. In particular, the clinical use of aminoglycoside antibiotics, broad-spectrum antibacterials of last resort, is limited due to rising bacterial resistance. One of the major resistance mechanisms in Gram-positive and Gram-negative bacteria is phosphorylation of these amino sugars at the 3’-position by O-phosphotransferases [APH(3’)s]. Structural alteration of these antibiotics at the 3’-position would be an obvious strategy to tackle this resistance mechanism. However, the access to such derivatives requires cumbersome multi-step synthesis, which is not appealing for pharma industry in this low-return-on-investment market. To overcome this obstacle and combat bacterial resistance mediated by APH(3’)s, we introduce a novel regioselective modification of aminoglycosides in the 3’-position via palladium-catalyzed oxidation. To underline the effectiveness of our method for structural modification of aminoglycosides, we have developed two novel antibiotic candidates overcoming APH(3’)s-mediated resistance employing only four synthetic steps. 相似文献
87.
Polymicrobial Biofilm Inhibition Effects of Acetate‐Buffered Chitosan Sponge Delivery Device 下载免费PDF全文
Jessica Amber Jennings Karen E. Beenken Ashley C. Parker James Keaton Smith Harry S. Courtney Mark S. Smeltzer Warren O. Haggard 《Macromolecular bioscience》2016,16(4):591-598
Polymicrobial biofilm‐associated implant infections present a challenging clinical problem. Through modifications of lyophilized chitosan sponges, degradable drug delivery devices for antibiotic solution have been fabricated for prevention and treatment of contaminated musculoskeletal wounds. Elution of amikacin, vancomycin, or a combination of both follows a burst release pattern with vancomycin released above minimum inhibitory concentration for Staphylococcus aureus for 72 h and amikacin released above inhibitory concentrations for Pseudomonas aeruginosa for 3 h. Delivery of a vancomycin, amikacin, or a combination of both reduces biofilm formation on polytetrafluoroethylene catheters in an in vivo model of contamination. Release of dual antibiotics from sponges is more effective at preventing biofilm formation than single‐loaded chitosan sponges. Treatment of pre‐formed biofilm with high‐dose antibiotic release from chitosan sponges shows minimal reduction after 48 h. These results demonstrate infection‐preventive efficacy for antibiotic‐loaded sponges, as well as the need for modifications in the development of advanced materials to enhance treatment efficacy in removing established biofilm.
88.
Illanes A Wilson L Caballero E Fernández-Lafuente R Guisán JM 《Applied biochemistry and biotechnology》2006,133(3):189-202
Crosslinked enzyme aggregates (CLEAs) of a partially purified penicillin acylase from a recombinant Escherichia coli strain have been produced as a novel type of biocatalysts well endowed to perform in organic media. Different protein precipitants
were studied and glutaraldehyde was used as the crosslinking agent. Precipitation curves were obtained for all precipitants
to determine the concentrations at which all the protein precipitated out of the solution. The effect of the glutaraldehyde-to-protein
ratio was studied with respect to process recovery and the specific activity and stability of the biocatalyst. Recovery of
penicillin acylase activity was moderately high, about 50%; major losses of enzyme activity were produced at the precipitation
step. Specific activities of all CLEAs were very high, which is one of the advantages of using nonsupported biocatalysts.
Ammonium sulfate and tert-butyl alcohol were the best precipitants at a glutaraldehyde-protein mass ratio of 2 and were selected to perform the kinetically
controlled synthesis of ampicillin in 60% (v/v) ethylene glycol medium. At comparable conversion yields, volumetric and specific
antibiotic productivity were much higher for CLEAs than for carrier-bound penicillin acylases. 相似文献
89.
90.
The major achievements of the G. F. Gauze Scientific-Research Institute of New Antibiotics, Russian Academy of Medical Sciences, over the last 50 years are reviewed. The structures of antibiotics and related compounds discovered at the Institute and important for medical practise and/or of theoretical interest as new compounds with high biological activity are described.Dedicated to the memory of Director of the G. F. Gauze Scientific-Research Institute of New Antibiotics, Russian Academy of Medical Sciences, and Corresponding Member of the Russian Academy of Medical Sciences Prof. Yu. V. Dudnik (1938–2003).Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1603–1618, November, 2004. 相似文献