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β-内酰胺

β-内酰胺的相关文献在1986年到2023年内共计3551篇,主要集中在药学、化学、化学工业 等领域,其中期刊论文212篇、会议论文22篇、专利文献47526篇;相关期刊143种,包括海峡药学、药物分析杂志、中国抗生素杂志等; 相关会议15种,包括2011年全国医药学术论文交流会、中华医学会第一届感染与抗微生物治疗论坛、第八届全国感染性疾病及抗微生物化疗学术会议、第19届全国儿科药学学术会议等;β-内酰胺的相关文献由6836位作者贡献,包括程时标、张树忠、谢丽等。

β-内酰胺—发文量

期刊论文>

论文:212 占比:0.44%

会议论文>

论文:22 占比:0.05%

专利文献>

论文:47526 占比:99.51%

总计:47760篇

β-内酰胺—发文趋势图

β-内酰胺

-研究学者

  • 程时标
  • 张树忠
  • 谢丽
  • 慕旭宏
  • 宗保宁
  • 闵恩泽
  • 杨克勇
  • 王皓
  • 范瑛琦
  • 吴望成
  • 期刊论文
  • 会议论文
  • 专利文献

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    • 王晓燕; 秦亚玲; 韩群; 辜锡恩; 晏紫; 付奎; 李德峰; 邓锴
    • 摘要: 具有多重耐药性和广泛耐药性的结核分枝杆菌菌株正在全球范围内传播,因此迫切需要新的抗结核药物.结核分枝杆菌的L,D-转肽酶LdtMt2直接参与肽聚糖的形成、细菌毒性和β-内酰胺抗性.该酶是潜在的抗结核靶标,可以被碳青霉烯类抗生素抑制,碳青霉烯类抗生素是FDA批准的用于治疗肺结核的药物.据报道,LdtMt2与碳青霉烯类抗生素(如厄他培南、亚胺培南和美洛培南)相互作用时,存在两种不同的中间状态,即状态Ⅰ和Ⅱ.状态Ⅰ被认为是初始加合物形成状态,而状态Ⅱ被认为是稳定的蛋白质-配体相互作用状态,并伴有碳青霉烯类抗生素和蛋白质的局部构象排列.本文报告了一个LdMt2-ertapenem新中间状态Ⅰ-plus,具有与状态Ⅱ相同的碳青霉烯类抗生素构象和与状态Ⅰ相似的局部蛋白质构象.该新状态是从状态Ⅰ转变为状态Ⅱ的中间状态,构象变化发生在厄他培南分子而不是蛋白质,我们的工作有助于阐明碳青霉烯类抗生素对LdtMt2作用后发生的变化,并与其他报道的中间状态一起揭示L,D-转肽酶如何与碳青霉烯类抗生素相互作用.
    • 罗静
    • 摘要: 目的 研究β-内酰胺类抗菌药物皮肤过敏试验阴性后过敏反应的规律与特点.方法 回顾性分析2017年1月~2018年10月本院收治的30例β-内酰胺类抗菌药物(主要为头孢类与青霉素类)皮肤过敏试验阴性后过敏反应住院患者,收集其临床资料,评估年龄、药品使用分类、过敏临床反应、过敏反应发生时间与缓解时间等.结果 年龄<1岁出现β-内酰胺类抗菌药物皮肤过敏试验阴性后过敏反应占比高达50.00%,均高于其他年龄段的比例,差异有统计学意义(P<0.05);占比前三药品为美洛西林(33.33%)、哌拉西林他唑巴坦(20.00%)以及头孢哌酮舒巴坦(13.34%);临床表现以瘙痒、风团、皮疹等为主,累及部位不固定;发生时间主要为7~9剂(用药4d后);12h以内缓解共19例(63.33%).结论 β-内酰胺类抗菌药物皮肤过敏试验阴性后过敏反应易发人群为<1岁,发生时间、发生部位均不固定,要求对患者使用β-内酰胺类抗菌药物过程中需严密监督观察.
    • XU Wei-long
    • 摘要: 文章通过头孢他啶侧链活性酯和(3S-反式)-3-氨基-4-甲基-2-氧代-1-氮杂环丁烷磺酸为主要原料先合成叔丁酯氨曲南,然后在酸性条件下水解获得α-氨曲南,再通过无水乙醇条件下转晶获得β-氨曲南,并对合成产物进行表征.实验结果表明,合成产物为β-氨曲南,理化性质均能达到国家药品要求.
    • 李辉; 张振
    • 摘要: 目的 分析儿童肠道双歧杆菌和乳酸杆菌对β-内酰胺/β-内酰胺酶抑制剂复合物(β-1actam/β-lactamase inhibitors)的药敏情况.方法 按照伯杰细菌鉴定手册的方法从36例健康儿童大便标本中分离出45株双歧杆菌和39株乳酸杆菌,依据2015年临床和实验室标准协会(CLSI)的标准,采用E-test方法实施双歧杆菌和乳酸杆菌对氨苄西林、阿莫西林/克拉维酸、氨苄西林/舒巴坦、哌拉西林、哌拉西林/他唑巴坦、替卡西林、替卡西林/克拉维酸、头孢哌酮、头孢哌酮/舒巴坦的药敏试验,并进行统计分析.结果 45株双歧杆菌对氨苄西林、阿莫西林/克拉维酸、氨苄西林/舒巴坦、哌拉西林、哌拉西林/他唑巴坦、替卡西林、替卡西林/克拉维酸、头孢哌酮敏感百分率分别为77.78%、95.56%、88.89%、73.33%、91.11%、68.89%、84.44%、82.22%,39株乳酸杆菌对上述抗生素敏感百分率分别为74.36%、94.87%、92.31%、71.79%、92.31%、69.23%、89.74%、79.49%.除头孢哌酮/舒巴坦没有CLSI药敏MIC解释标准而无法判断外,其他β-lactam/β-lactamase inhibitor均比单一β-lactam抗生素敏感百分率升高,双歧杆菌氨苄西林与阿莫西林/克拉维酸、哌拉西林与哌拉西林/他唑巴坦的敏感数P值分别为0.01、0.03,乳酸杆菌氨苄西林与阿莫西林/克拉维酸、氨苄西林与氨苄西林/舒巴坦、哌拉西林与哌拉西林/他唑巴坦、替卡西林与替卡西林/克拉维酸的敏感数P值分别为0.01、0.03、0.02、0.03.结论 β-lactam/β-lactamase inhibitor比单一β-lactam抗生素抑制儿童肠道双歧杆菌和乳酸杆菌作用更强.%Objective To analyze the susceptibility situation of bifidobacteria and lactobacilli from child intestinal tract on β-lactam/β-lactamase inhibitor complex.Methods According to the method of the Bergey Bacterial Identification Manual,45 strains of bifidobacteria and 39 strains of lactobacilli were isolated from the stool specimens of 36 healthy children.The susceptibility tests of bifidobacteria and lactobacilli to ampicillin,amoxicillin/clavulanate,ampicillin/sulbactam,piperacillin,piperacillin/tazobactam,ticarcillin,ticarcillin/clavulanate,cefoperazone and cefoperazone/sulbactam were performed by adopting the E-test method.Then the statistical analysis was conducted.Results The sensitivity percentages of 45 strains of bifidobacteria to ampicillin,amoxicillin/clavulanate,ampicillin/sulbactam,piperacillin,piperacillin/tazobactam,ticarcillin,ticarcillin/clavulanate and cefoperazone were 77.78%,95.56%,88.89%,73.33%,91.11%,68.89%,84.44% and 82.22% respectively,which of 39 strains of lactobacilli to above antibiotic drugs were 74.36%,94.87%,92.31%,71.79%,92.31%,69.23%,89.74% and79.49%,respectively.Except having no judgment due to without the CLSI drug susceptibility MIC interpretation criteria of cefoperazone/sulbactam,the sensitivity percentages of other β-lactam/β-lactamase inhibitor complex were higher than those of single β-lactam antibi otics,the sensitive number P values of bifidobacteria in ampicillin with amoxicillin/clavulanate and piperacillin with piperacillin/tazobactam were 0.01 and 0.03 respectively,which of lactobacilli in ampicillin with amoxicillin/clavulanate,ampicillin with ampicillin/sulbactam,piperacillin with piperacillin/tazobactam,ticarcillin with ticarcillin/clavulanate were 0.01,0.03,0.02 and 0.03 respectively.Conclusion β-lactam/β-lactamase inhibitors complex has stronger effect for inhibiting child intestinal tract bifidobacteria and lactobacilli than single β-lactam antibiotics.
    • 周敏; 徐小英; 龙远德
    • 摘要: 以羧甲基-β-环糊精为手性固定相填料,建立了反相高效液相色谱拆分17种顺式-β-内酰胺的方法.考察了流动相pH值、盐种类和浓度及流动相组成对分离效果的影响.选定的流动相为(0.10%NH4Ac+FA)(pH=5.0)-MeOH(体积比70:30),在此条件下,17个 β-内酰胺化合物中有7个化合物的分离度>1.5,4个化合物的分离度在1.0~1.5之间,其余化合物的分离度<1.0.理论拆分机理研究结果表明,羧甲基-β-环糊精手性拆分过程是环糊精的包结作用与氢键、偶极相互作用和立体位阻等作用力协同作用的过程.与未衍生的环糊精手性固定相相比,羧甲基-β-环糊精手性固定相具有更好的分离效果.%A reversed phase high performance liquid chromatographic method was developed using carboxymethyl-β-cyclodextrin chiral stationary phase for enantioseparation of seventeen kinds of cis-β-lactams enantiomers. Most of the compounds could get base-line separation. The effects of mobile phase pH, salt type and concentration, as well as mobile phase proportion were discussed. The results showed that ( 0. 10%NH4 Ac+FA ) ( pH= 5. 0 )-MeOH ( 70 : 30, volume ratio ) was the optimum condition for most of chiral compound. Under the optimum condition, the 7 compounds for CA series could get base-line separation except for compound 18CA, the best resolution values for compounds 15CA and 17CA were 1. 71 and 1. 74, respectively. The resolution values for seven EA compounds were between 1. 00 and 1. 50 which was nearly close to base-line separation except for compounds 18EA and 22EA. The resolution values for three BA compounds were close to 1. 00. Structures of analytes also played important role in chiral separation. The results indicated that better resolution could be obtained if the analyte with proper size matching cyclodextrin cavity. Hydrogen bond interaction between the substituents on the cyclodextrin derivative and the analytes and smaller steric hindrance were also good for enantioseparation. Smaller steric hindrance making analytes easily penetrate into cyclodextrin cavity was beneficial to enantioseparation. A tentative chiral recognition mechanism was proposed after a comprehensive analysis of the influencing factors for enantioseparation using compound 15CA as example. Inclusion interaction, hydrogen bond interaction, dipole-dipole interaction and steric hindrance were found to exert synergistic effects on enantioseparation. However, the inclusion interaction between the analytes and the cyclodextrin was the primary role for enantioselective recognition. In comparison with native β-CD CSP , CM-β-CD CSP exhibited enhanced enantioseparation.
    • 周鑫; 张立田; 项爱丽; 郑百芹; 李爱军
    • 摘要: 采用液质联用仪法测定生鲜乳中5种β-内酰胺类抗生素的残留量.试验结果表明,5种β-内酰胺类药物在5~100 ng/mL的浓度范围内,其回归标准曲线方程的相关系数为0.9923~0.9998,回收率在65.6%~102.2%范围内,变异系数为3.45%~9.23%.本试验为大批量生鲜乳样品的β-内酰胺类药物的检测提供了一种有效方法.
    • 姚飞飞; 崔巍; 肖德海; 张吉凤
    • 摘要: 阿莫西林是一种最常用的β-内酰胺抗生素,作为基本医疗系统中最重要药物之一被世界卫生组织基本药物标准清单收录. 其杂质L,即:(2S,5R,6R)-6-((2S,5R,6R)-6-((R)-2-氨基-2-(4-羟基苯基)乙酰氨基)-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酰胺)-3,3-二甲基-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸(6-APA amoxicillin amide),由于含量少难以获取成为影响产品质量的因素之一,因此,我们以6-氨基青霉素烷酸和阿莫西林三水合物为原料,分别通过3步和1步转化为相应的中间体化合物3和6,并使用酰胺缩合试剂六氟磷酸苯并三唑-1-基-氧基三吡咯烷基磷(PyBOP)以76%的收率实现了化合物3和6的脱水缩合,得到的关键中间体化合物7在Pd/C催化条件下一步脱除苄基及两个苄氧羰基保护基,首次通过化学方法合成了β-内酰胺化合物阿莫西林杂质L,反应使用简单易得的原料,温和的反应条件,无需复杂的分离纯化处理,对以阿莫西林为代表的β-内酰胺类抗生素的过敏研究以及新型β-内酰胺抗生素的开发和作用机制研究等有着参考和借鉴意义.%Amoxicillin is a β-lactam antibiotic used for the treatment of a number of bacterial infections.It is on the World Health Organization′s List of Essential Medicines, and one of the most important medications needed in a basic health system.The insufficient sources of its impurity L, i.e., (2S,5R,6R)-6-((2S,5R,6R)-6-((R)-2-amino-2-(4-hydroxyphenyl)acetamido)-3,3-dime-thyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicy-clo[3.2.0]heptane-2-carboxylic acid(6-APA amoxicilin amide), affect the quality control of the product.Herein, the first synthesis of amoxicillin impurity L, was reported by using a simple and efficient method.The starting materials of 6-aminopenicilanic acid and amoxycillin trihydrate were converted to intermediate compounds 3 and 6 through three-step and one-step reactions, respectively.By using benzotriazole-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate(PyBOP) as peptide coupling reagent, we successfully synthesized key intermediate 7 from compounds 3 and 6 in 76% yield, which was subsequently transformed to 6-APA amoxicillin amide by fully deprotection of benzyl and two carbobenzyloxy(Cbz) protecting groups.This method not only increases the source of the standard substance for quality control of amoxicillin, but also provides inspiration for novel β-lactam antibiotic and antiallergic research.
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