CAS: 84305-41-9; (6R,7S)-7-(2-(((S)-2-Amino-2-Carboxyethyl)Thio)Acetamido)-7-Methoxy-3-(((1-Methyl-1H-Tetrazol-5-yl)Thio)Methyl)-8-Oxo-5-Thia-1-Azabicyclo[4.2.0]Oct-2-Ene-2-Carboxylic Acid

该化合物是一种属于乙型乳腺抗生素类的半合成性脑膜骨灰质素抗生素,主要用于治疗各种细菌感染,特别是由抗抗菌素和某些抗菌素细菌造成的细菌感染;Cefminox具有广泛的活动范围,能够有效防治某些Echerichia coli,Klebsiella和其他病原体的菌株;通过抑制细菌细胞墙合成合成,导致细胞分解和死亡,复合物的工作,通常通过注射进行,并因其稳定性而为人所知,因为某些乙型乳腺是某些细菌生成的酶,这些细菌对其他抗生素具有抗药性;Cefminox经常用于临床环境中呼吸道,皮肤和软组织感染,以及腹部感染;与所有抗生素一样,其使用应以感应测试为指导,以确保有效性和尽量减少抗药性;潜在的副作用包括过敏反应,胃肠道扰动和血液参数变化.

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      专利信息


      专利号:US-9353057-B2
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
      发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
      权利人:XENOPORT INC
      摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

      专利号:US-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:US-2009111737-A1
      优先权日:1999-05-24
      标题:Novel antibacterial agents
      发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
      权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES
      摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.

      专利号:WO-2009094569-A2
      优先权日:2008-01-25
      标 题:Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates

      专利号:US-2025002508-A1
      优先权日:2020-05-05
      标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
      发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
      权利人:QPEX BIOPHARMA INC
      摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

      专利号:US-2005222431-A1
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

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      主要参考文献


      1: Xia J, Yang L, Dong L, Niu M, Zhang S, Yang Z, Wumaier G, Li Y, Wei X, Gong Y, Zhu N, Li S. Cefminox, a Dual Agonist of Prostacyclin Receptor and Peroxisome Proliferator-Activated Receptor-Gamma Identified by Virtual Screening, Has Therapeutic Efficacy against Hypoxia-Induced Pulmonary Hypertension in Rats. Front Pharmacol. 2018 Feb 23;9:134. doi: 10.3389/fphar.2018.00134.
      2: Xu Y, Wang D, Tang L, Wang J. Separation and Characterization of Unknown Impurities and Isomers in Cefminox Sodium and Study of the Forming Mechanisms of Impurities by Liquid Chromatography Coupled with Ion Trap/Time-Of-Flight Mass Spectrometry. J Chromatogr Sci. 2019 Mar 1;57(3):204-212. doi: 10.1093/chromsci/bmy101. 13(6):317-25. doi: 10.2165/00044011-199713060-00004. 42(3):495-501.
      5: Hilali A, Jiménez JC, Callejón M, Bello MA, Guiraúm A. Electrochemical reduction of cefminox at the mercury electrode and its voltammetric determination in urine. Talanta. 2003 Jan 2;59(1):137-46. doi: 10.1016/s0039-9140(02)00468-x. 33(2):372-4. doi: 10.1093/jac/33.2.372. 182(2):313-7. doi: 10.1111/j.1574-6968.2000.tb08914.x. 9(7):e103253. doi: 10.1371/journal.pone.0103253.

      合成参考文献


      参考文献:10.1007/bf01743360
      摘要:Van Vlem B, Vanholder R, De Paepe P, Vogelaers D, Ringoir S. Immunomodulating effects of antibiotics: literature review. Infection. 1996 Jul;24(4):275–91. doi: 10.1007/bf01743360.
      参考文献:10.1007/s101560200022
      摘要:Kumazawa J, Yagisawa M. The history of antibiotics: the Japanese story. J Infect Chemother. 2002 Jun;8(2):125–33. doi: 10.1007/s101560200022.
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