CAS: 120138-50-3; Quinupristin

该化合物是一种半合成抗生素,属于抗生素链状菌类,主要与dalfopristin结合使用,用于治疗包括抗肠道菌菌在内的抗乳细胞细菌引起的严重感染.它的作用是禁止细菌蛋白合成,具体针对50S 脊髓膜炎子细胞.Quinupristin展示了各种病原体的多种活动,使其有效地治疗皮肤和软组织感染以及复杂的腹内感染等病症.该化合物以其独特的行动机制著称,该机制涉及与不同地点结合的脊髓膜炎,在与dalfopristin结合使用时产生协同效应.Quinupristin通常进行静脉注射,可能会产生副作用,如胃肠紊乱和潜在的肝中毒.它通常保留用于其他抗抗药无效的病例,突出其在抗抗生素抗菌细菌抗药性斗争中的重要性.

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      专利信息


      专利号:US-10925977-B2
      优先权日:2006-10-05
      标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
      发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
      权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
      摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

      专利号:US-2024197774-A1
      优先权日:2021-04-16
      标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
      发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
      权利人:UNIV TEXAS
      摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

      专利号:US-9982005-B2
      优先权日:2013-04-04
      标 题 :Macrolides and methods of their preparation and use
      发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
      权利人:HARVARD COLLEGE
      摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

      专利号:US-10899773-B2
      优先权日:2014-12-19
      标 题 :Total synthesis of trioxacarcin DC-45-A2 and preparation of trioxacarcin analogs
      发明人:NICOLAOU KYRIACOS C; CAI QUAN
      权利人:UNIV RICE WILLIAM M
      摘要:In one aspect, the present invention provides novel derivatives of trioxacarin analogs of the formula (I) wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.

      专利号:US-2016185745-A1
      优先权日:2013-08-07
      标题:Analogs of vinaxanthone and xanthofulvin, methods of synthesis, and methods of treatments thereof
      发明人:SIEGEL DIONICIO; CHIN MATTHEW; ELIASEN ANDERS; AXELROD ABRAM
      权利人:UNIV TEXAS
      摘要:The present invention relates generally to methods of synthesis of vinaxanthone and xanthofulvin, novel analogs, and methods of use thereof.

      专利号:US-11466046-B2
      优先权日:2014-10-08
      标题 :14-membered ketolides and methods of their preparation and use
      发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
      权利人:HARVARD COLLEGE
      摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

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      主要参考文献


      1: Maraki S, Samonis G, Dimopoulou D, Mantadakis E. Susceptibility of Glycopeptide-Resistant Enterococci to Linezolid, Quinupristin/dalfopristin, Tigecycline and Daptomycin in a Tertiary Greek Hospital. Infect Chemother. 2014 Dec;46(4):253-6. doi: 10.3947/ic.2014.46.4.253. Epub 2014 Dec 29.
      2: Yu F, Lu C, Liu Y, Sun H, Shang Y, Ding Y, Li D, Qin Z, Parsons C, Huang X, Li Y, Hu L, Wang L. Emergence of quinupristin/dalfopristin resistance among livestock-associated Staphylococcus aureus ST9 clinical isolates. Int J Antimicrob Agents. 2014 Nov;44(5):416-9. doi: 10.1016/j.ijantimicag.2014.06.020. Epub 2014 Aug 17. doi: 10.3967/bes2014.065. doi: 10.1089/mdr.2012.0176. Epub 2013 Feb 26. doi: 10.4103/0377-4929.116164. doi: 10.1001/archophthalmol.2012.1504. doi: 10.1016/j.mcna.2011.03.011. doi: 10.1186/1752-1947-5-130.
      9: Hwang IY, Ku HO, Lim SK, Lee KJ, Park CK, Jung GS, Jung SC, Park YH, Nam HM. Distribution of streptogramin resistance genes and genetic relatedness among quinupristin/dalfopristin-resistant Enterococcus faecium recovered from pigs and chickens in Korea. Res Vet Sci. 2010 Aug;89(1):1-4. doi: 10.1016/j.rvsc.2010.01.011. Epub 2010 Mar 5. doi: 10.3109/00365541003699623. doi: 10.1093/jac/dkq110. Epub 2010 Apr 8. doi: 10.1016/j.diagmicrobio.2008.06.004. Epub 2008 Jul 23. doi: 10.1016/j.idc.2009.06.010. Review. doi: 10.1016/j.ijantimicag.2009.03.018. Epub 2009 May 5. doi: 10.1111/j.1469-0691.2008.01993.x. Epub 2008 Apr 5. doi: 10.1007/s12275-007-0217-1. Epub 2007 Dec 3.

      合成参考文献


      参考文献:10.1128/aac.43.8.2043
      摘要:Khan AA, Slifer TR, Araujo FG, Remington JS. Quinupristin-Dalfopristin Is Active against Toxoplasma gondii. Antimicrob Agents Chemother. 1999 Aug;43(8):2043–5. doi: 10.1128/aac.43.8.2043.
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