以γ-环糊精和D-苯丙氨酸为手性选择剂,采用毛细管区带电泳成功地分离了新型抗菌素西他沙星差向异构体。考察了添加剂的种类、浓度和缓冲溶液的pH对毛细管电泳分离西他沙星的影响。分离电压为15kV,选用60cm(有效长度52.5cm)×50μm ...以γ-环糊精和D-苯丙氨酸为手性选择剂,采用毛细管区带电泳成功地分离了新型抗菌素西他沙星差向异构体。考察了添加剂的种类、浓度和缓冲溶液的pH对毛细管电泳分离西他沙星的影响。分离电压为15kV,选用60cm(有效长度52.5cm)×50μm i.d.的石英毛细管,缓冲溶液组成为10mm o l/L KH2PO4-K2HPO4(pH4.5),10mm o l/L C uSO4,20mm o l/Lγ-环糊精和10mm o l/LD-苯丙氨酸。实验结果表明,添加剂的种类和浓度是影响西他沙星手性分离的重要因素,只有当D-苯丙氨酸、铜离子和γ-环糊精同时存在并达到一定浓度时,西他沙星差向异构体在毛细管电泳中才具有良好的分离效果。该方法可用于西他沙星差向异构体的定量分析。展开更多
Helicobacter pylori is a highly successful bacterium with a high global prevalence and the infection carries significant disease burden. It is also becoming increasingly difficult to eradicate and the main reason for ...Helicobacter pylori is a highly successful bacterium with a high global prevalence and the infection carries significant disease burden. It is also becoming increasingly difficult to eradicate and the main reason for this is growing primary antibiotic resistance rates in a world where antibiotics are frequently prescribed and readily available. Despite knowing much more about the bacterium since its discovery, such as its genomic makeup and pathogenesis, we have seen declining treatment success. Therefore, clinicians today must be prepared to face one, two or even multiple treatment failures, and should be equipped with sufficient knowledge to decide on the appropriate salvage therapy when this happens. This article discusses the factors contributing to treatment failure and reviews the second and thirdline treatment strategies that have been investigated. Established empiric second line treatment options include both bismuth based quadruple therapy and levofloxacin based triple therapy. Antibiotic testing is recommended prior to initiating third line treatment. In the event that antibiotic susceptibility testing is unavailable, third line treatment options include rifabutin, rifaximin and sitafloxacin based therapies.展开更多
Third generation of quinolones,such as levofloxacin and moxifloxacin,-containing regimens are often used in second-line or rescue treatment of Helicobacter pylori infection.However,the increasing antibiotic resistance...Third generation of quinolones,such as levofloxacin and moxifloxacin,-containing regimens are often used in second-line or rescue treatment of Helicobacter pylori infection.However,the increasing antibiotic resistance to quinolones affects the efficacies of quinolones-containing therapies in recent years.Therefore,there is a need to enhance the effectiveness of quinolonescontaining therapies.Sitafloxacin,a fourth-generation quinolone,and vonoprazan,a novel potassium-competitive acid blocker,are now available as more effective treatment options.The aim of this paper is to summarize the current evidence of quinolone-containing therapies in rescue treatments,and to discuss the importance of drug sensitivity tests or analysis of gyrA mutation before treatments.展开更多
A new compound [C19H19N3O3F2Cl·C4H3O4·H2O]（I）,（7-（（7S）-7-aminospiro[2.4]heptan-5-yl）-8-chloro-6-fluoro-1-（（1R,2S）-2-fluorocyclopropyl）-4-oxo-1,4-dihydroquinoline-3-carboxylic acid fumaric acid mon...A new compound [C19H19N3O3F2Cl·C4H3O4·H2O]（I）,（7-（（7S）-7-aminospiro[2.4]heptan-5-yl）-8-chloro-6-fluoro-1-（（1R,2S）-2-fluorocyclopropyl）-4-oxo-1,4-dihydroquinoline-3-carboxylic acid fumaric acid monohydrate）, was synthesized and structurally characterized by single-crystal X-ray diffraction, ^1H NMR, 14 C spectra and mass spectra. I crystallizes in monoclinic, space group P21/c with a = 8.495（2）, b = 12.545（3）, c = 11.832（3） A, β = 103.37（1）°, V = 1226.8（5） A^3, Z = 2, Mr = 543.90, Dc = 1.472 g/cm^3, F（000） = 564, μ = 0.225 mm^-1, the final R = 0.0307 and wR = 0.0892 for 6886 observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals that the quinolinone ring is almost coplanar, and the pyrrole ring adopts an envelope form. Packing of crystal I is constructed and stabilized by the N–H…O, O–H…O and N–H…Cl hydrogen bonds together with C–H…π interations.展开更多
文摘以γ-环糊精和D-苯丙氨酸为手性选择剂,采用毛细管区带电泳成功地分离了新型抗菌素西他沙星差向异构体。考察了添加剂的种类、浓度和缓冲溶液的pH对毛细管电泳分离西他沙星的影响。分离电压为15kV,选用60cm(有效长度52.5cm)×50μm i.d.的石英毛细管,缓冲溶液组成为10mm o l/L KH2PO4-K2HPO4(pH4.5),10mm o l/L C uSO4,20mm o l/Lγ-环糊精和10mm o l/LD-苯丙氨酸。实验结果表明,添加剂的种类和浓度是影响西他沙星手性分离的重要因素,只有当D-苯丙氨酸、铜离子和γ-环糊精同时存在并达到一定浓度时,西他沙星差向异构体在毛细管电泳中才具有良好的分离效果。该方法可用于西他沙星差向异构体的定量分析。
文摘Helicobacter pylori is a highly successful bacterium with a high global prevalence and the infection carries significant disease burden. It is also becoming increasingly difficult to eradicate and the main reason for this is growing primary antibiotic resistance rates in a world where antibiotics are frequently prescribed and readily available. Despite knowing much more about the bacterium since its discovery, such as its genomic makeup and pathogenesis, we have seen declining treatment success. Therefore, clinicians today must be prepared to face one, two or even multiple treatment failures, and should be equipped with sufficient knowledge to decide on the appropriate salvage therapy when this happens. This article discusses the factors contributing to treatment failure and reviews the second and thirdline treatment strategies that have been investigated. Established empiric second line treatment options include both bismuth based quadruple therapy and levofloxacin based triple therapy. Antibiotic testing is recommended prior to initiating third line treatment. In the event that antibiotic susceptibility testing is unavailable, third line treatment options include rifabutin, rifaximin and sitafloxacin based therapies.
文摘Third generation of quinolones,such as levofloxacin and moxifloxacin,-containing regimens are often used in second-line or rescue treatment of Helicobacter pylori infection.However,the increasing antibiotic resistance to quinolones affects the efficacies of quinolones-containing therapies in recent years.Therefore,there is a need to enhance the effectiveness of quinolonescontaining therapies.Sitafloxacin,a fourth-generation quinolone,and vonoprazan,a novel potassium-competitive acid blocker,are now available as more effective treatment options.The aim of this paper is to summarize the current evidence of quinolone-containing therapies in rescue treatments,and to discuss the importance of drug sensitivity tests or analysis of gyrA mutation before treatments.
基金Project supported by the National Natural Science Foundation of China(No.21272086)
文摘A new compound [C19H19N3O3F2Cl·C4H3O4·H2O]（I）,（7-（（7S）-7-aminospiro[2.4]heptan-5-yl）-8-chloro-6-fluoro-1-（（1R,2S）-2-fluorocyclopropyl）-4-oxo-1,4-dihydroquinoline-3-carboxylic acid fumaric acid monohydrate）, was synthesized and structurally characterized by single-crystal X-ray diffraction, ^1H NMR, 14 C spectra and mass spectra. I crystallizes in monoclinic, space group P21/c with a = 8.495（2）, b = 12.545（3）, c = 11.832（3） A, β = 103.37（1）°, V = 1226.8（5） A^3, Z = 2, Mr = 543.90, Dc = 1.472 g/cm^3, F（000） = 564, μ = 0.225 mm^-1, the final R = 0.0307 and wR = 0.0892 for 6886 observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals that the quinolinone ring is almost coplanar, and the pyrrole ring adopts an envelope form. Packing of crystal I is constructed and stabilized by the N–H…O, O–H…O and N–H…Cl hydrogen bonds together with C–H…π interations.
