CAS: 76610-84-9; Cefbuperazone

该化合物是一种第二代甲状腺素抗生素,其活动范围广泛,可以防治克氏阳性细菌和克氏阴性细菌,其化学结构包括一个β-乳性环,对许多β-乳性动物具有稳定性,提高了抗抗抗菌菌菌株的功效.Cefbuperazone 表现出强烈的细菌杀菌效应,特别是对诸如Sphylococcus aureus,Escherichia coli和Klebsiella肺炎等病原体.其药理学特征包括良好的组织渗透和长期半衰期,允许较少频繁的剂量.该化合物经常用于临床环境治疗呼吸道,尿道和腹内感染.其平衡的频谱和抗酶降解性使它成为实验性和有针对性的抗生素疗法的可靠选择.

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      专利号:US-8017776-B2
      优先权日:2003-07-15
      标题 :Methods for synthesis of acyloxyalkyl compounds
      发明人:BHAT LAXMINARAYAN; GALLOP MARK A
      权利人:XENOPORT INC
      摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.

      专利号:US-9693999-B2
      优先权日:2011-01-26
      标题:Small molecule RNase inhibitors and methods of use
      发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
      权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
      摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

      专利号:US-8143437-B2
      优先权日:2002-02-19
      标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
      发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X
      权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC
      摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.

      专利号:WO-0032619-A1
      优先权日:1998-11-30
      标题:Methods and compositions for identification of inhibitors of ribosome assembly
      发明人:DAMMEL CAROL S; WATSON JULIE C
      权利人:RIBOGENE INC
      摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.

      专利号:WO-2009056955-A1
      优先权日:2007-10-30
      标题 :Amine-bearing phospholipids (abps), their synthesis and use
      发明人:ZUMBUEHL ANDREAS
      权利人:UNIV BASEL; ZUMBUEHL ANDREAS
      摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

      专利号:US-9868747-B2
      优先权日:2014-02-18
      标题:Marinopyrrole derivatives and methods of making and using same
      发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI
      权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD
      摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.
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      主要参考文献


      1: Liu D, Geng T, Wang Y, Ding L. Pharmacokinetic profile of cefbuperazone in healthy Chinese volunteers after single and multiple drip intravenous infusion by HPLC-MS/MS. J Pharm Biomed Anal. 2016 Sep 10;129:28-33. doi: 10.1016/j.jpba.2016.06.029. Epub 2016 Jun 23. 4(6):415-23. 27(4):640-2. doi: 10.1128/aac.27.4.640.
      4: Suzuki I, Senda H, Yokota T. In vivo activity of cefbuperazone (T-1982) against various experimental infections in mice. J Antibiot (Tokyo). 1985 Feb;38(2):249-58. doi: 10.7164/antibiotics.38.249. 11(9):577-84. 27(5):817-20. doi: 10.1128/aac.27.5.817.
      7: Kager L, Brismar B, Malmborg AS, Nord CE. Impact of cefbuperazone on the colonic microflora in patients undergoing colorectal surgery. Drugs Exp Clin Res. 1986;12(12):983-6. 4(2):150-3. 26(4):585-90. doi: 10.1128/aac.26.4.585.

      合成参考文献


      参考文献:10.3412/jsb.42.757
      摘要:Inada K, Kumagai K, Matui S, Suzuki M, Yoshida M. [Stimulation of human T lymphocyte colony formation by cefbuperazone and other beta-lactam antibiotics]. Nihon Saikingaku Zasshi. 1987 Sep;42(5):757–62. doi: 10.3412/jsb.42.757.
      摘要:S6 | ITNANTIBIOTIC | Antibiotic List from the ITN MSCA ANSWER | DOI:10.5281/zenodo.2621956
      摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2003).
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