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噁唑烷酮类抗菌药物研究进展 被引量：5

Progress in the research of novel oxazolidinone antibacterial agents
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摘要 抗生素的广泛使用使得细菌的耐药性问题日益严重,新型抗耐药菌药物的研究已成为抗菌药物研究的主要方向。其中,全合成的噁唑烷酮类抗菌药物利奈噁唑酮已成功上市,并取得了良好的临床治疗效果,这促使了对该类化合物更为深入的研究。本文对噁唑烷酮类抗菌剂的作用机制、耐药机制、结构修饰进行综述,并着重介绍了近年来具有优良抗菌活性的噁唑烷酮类潜在药物。 Since the widespread use of antibiotics has led to the severe rising tide of bacterial resistance, the exploration of new antibacterial drugs has become a crucial part in nowadays researches. The success of lin- ezolid--one typical oxazolidinones drug with potent therapeutic effect has become the impetus for oxazolidi- none to be deeply improved upon going forward. The mechanism of action, the mechanism of resistance and the structural modification of oxazolidinone antibacterial drugs were reviewed. Furthermore, the introduction of potential drugs which were found to possess excellent antibacterial activity in recent years was highly emphasized.
作者 王吕鸣 刘敏 沈思思 沙宇
机构地区 沈阳药科大学基于靶点的药物设计与研究教育部重点实验室
出处 《中国药物化学杂志》 CAS CSCD 2013年第3期218-225,共8页 Chinese Journal of Medicinal Chemistry
基金 辽宁省教育厅资助项目(2009226015-5)
关键词 噁唑烷酮 利奈唑酮 耐药机制 结构修饰 抗菌活性 oxazolidinone linezolid resistance mechanism structural modification antibacterial activity
分类号 R914 [医药卫生—药物化学]
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参考文献28

  • 1AMENT P W, JAMSHED N, HORNE J P. Linezo- lid:its role in the treatment of Gram-positive, drug- resistant bacterial infections [ J]. Am Fam Physician, 2002,65 (4) : 663 - 671.
  • 2LI Z, WILLKE R J, PINTO L A, et al. Comparison of length of hospital stay for patients with known or suspected methicillin-resistant Staphylococcus species infections treated with linezolid or vancomycin: a randomized, multicenter trial [ J ]. Pharmacotherapy, 2001,21 ( 3 ) :263 - 274.
  • 3SHINABARGER D. Mechanism of action of the ox- azolidinone antibacterial agents [ J ]. Exp Opin Invest Drugs, 1999,8 ( 8 ) : 1195 - 1202.
  • 4ZHOU C C, SWANEY S M, SHINABARGER D L, et al. 1H nuclear magnetic resonance study of oxazo- lidinone binding to bacterial ribosomes[ J ]. Antimi- crob Agents Chemother,2002,46( 3 ) :625 - 629.
  • 5PATEL U, YAN Y P, HOBBS F W, et al. Oxazolidi- nones mechanism of action:inhibition of the first peptide bond formation[ J ]. J Biol Chem,2001,276 (40) :37199 - 37205.
  • 6IPPOLITO J A, KANYO Z F, WANG D P, et al. Crystal structure of the oxazolidinone antibiotic linezolid bound to the 50S ribosomal subunit [ J ]. J Med Chem,2008,51 (12) :3353 -3356.
  • 7WILSON D N, SCHLUENZEN F, HARMS J M, et al. The oxazolidinone antibiotics perturb the riboso- mal peptidyl-transferase center and effect tRNA posi-tioning [ J ] Proc Natl Acad Sci USA, 2008, 105 (36) :13339 - 13344.
  • 8LIVERMORE D M ,WARNER M ,MUS HTAQ S ,et al. In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and susceptible Staphylo- cocci and Enterococci [ J ]. Antimicrob Agents Che- mother,2007,51 (3) :1112 - 1114.
  • 9SLEE A M, WUONOLA M A, MCRIPLEY R J, et al. Oxazolidinones, a new class of synthetic antibac- terial agents: in vitro and in vivo activities of DuP 105 and DuP 721[ J ] Antimicrob Agents Chemoth- er,1987,31 ( 11 ) : 1791 - 1797.
  • 10BRICKNER S J,HUTCHINSON D K,BARBACHYN M R,et al. Synthesis and antibacterial activity of U- 100592 and U-100766,two oxazolidinone antibacteri- al agents for the potential treatment of multidrug-re- sistant Gram-positive bacterial infections [ J ]. J Med Chem. 1996.39 ( 3 ) 673 - 679.

二级参考文献28

  • 1Poulakou G, Giamarellou H. Investigational treatments for postoperative surgical site infections [J]. Expert Opin Investig Drugs, 2007, 16(2): 137-55.
  • 2Sood R, Bhadauriya T, Rao M, et al. Antimycobacterial activities of oxazolidinones: a review [J]. Infect Disord Drug Targets, 2006, 6(4): 343-54.
  • 3Howe RA, Woottonet M, Noel AR, et al. Activity of AZD2563, a novel oxazolidinone, against staphylococcus aureus strains with reduced susceptibility to vancomycin or linezolid[.l]. Antimicrob Agents Chemother, 2003, 47 (11): 3651-52.
  • 4Johnson AP. AZD-2563 AstraZeneca [J]. Curr Opin Investig Drugs, 2002, 3(6): 848-52.
  • 5Fluit AC, Schmitz FJ, Verhoef J, et al. In vitro activity of AZD2563, a novel oxazolidinone, against European Gram-positive cocci [J]. J Antimicrob Chemother, 2002, 50(2): 271-6.
  • 6Stockdale MW, Woodford N, Tysall L, et al. Low in vitro selection frequencies of enterococcal and Staphylococcal mutants resistant to the oxazolidinone AZD2563[J]. Int J Antimicrob Agents, 2004, 23(1): 88-91.
  • 7Kalia V, Miglani R, Raj VS, et al. Mode of action of Ranbezolid against Staphylococci and structural modeling studies of its interaction with ribosomes[J]. Antimicrob Agents Chemother, 2009, 53(4): 1427-33.
  • 8Das B, Rudra S, Yadav A, et al. Synthesis and SAR of novel oxazolidinones: Discovery of ranbezolid [J]. Bioorg Med Chem Lett, 2005, 15(19): 4261-7.
  • 9Yoon EJ, Jo YW, Choi SH, et al. In vitro and in vivo activities of DA-7867, a new oxazolidinone, against aerobic gram-positive bacteria [J]. Antimicrob Agents Chemother, 2005, 49(6): 2498-500.
  • 10Vera-Cabrera L, Gonzalez E, Choi SH, et al. In vitro activities of new antimicrobials against nocardia brasiliensis[J]. Antimicrob Agents Chemother, 2004, 48 (2): 602-4.

共引文献19

同被引文献41

  • 1陈新谦,金有豫,汤光.新编药物学(第17版).北京:人民卫生出版社.2011.
  • 2耐甲氧西林金黄色葡萄球菌感染防治专家委员会.耐甲氧西林金黄色葡萄球菌感染防治专家共识[J].中华实验和临床感染病杂志,2011;5(3):372-384.
  • 3Birmingham MC,Rayner CR, Meagher AK,et al. Linezolid for the treatment of multidrug-resistant,grampositive infections: experience from a compassionate-use program [J]. Clin Infect Dis,2003;36(2):159-168.
  • 4Matsumoto K,Takeshita A,Ikawa K,et al.Higher linezolid exposure and higher frequency of thrombocytopenia in patients with renal dysfunction [J]. Int J Antimicrob Agents2010;36(2): 179-181.
  • 5Matsumoto K,Takeda Y, Takeshita A,et al. Renal function as a predictor of lineolid-inuced thrombocytopenia [J]. Int J Antimicrob Agents,2009;33( 1):98-99.
  • 6BERLIN K D, SCHERLAG B J, CLARKE C R, et al. Salts of 3-azabicyclo E 3. 3. 1 ] nonanes as anti- arrhythmic agents, and precursors thereof: 9107405 [ P]. 1991 - 05 - 30.
  • 7HESTER J B, NIDY E G, PERRICONE S C, et al. Oxazolidinone antibacterial agents having a thio- carbonyl functionality: 2000032599 [ P ]. 2000 - 06 - 08.
  • 8TAYLOR P, RADIC Z, SHARPLESS K B, et al. Centrally active and orally bioavailable antidotes for organophosphate exposure and methods for making and using them :2014127315 [ P]. 2014 - 08 - 21.
  • 9CHEN B, FAIRHURST R A, FLOERSHEIMER A, et al. Ether derivatives of bicyclic heteroaryls: 2011029915 [ P]. 2011 - 03 - 17.
  • 10MAGEE D I, BECK E J. Use of the Ramberg- bicklund rearrangement for the synthesis of medium and large heterocyclic alkenes: stereoselective olefin formation[ J]. J Org Chem, 2000,65 (24) : 8367 - 8371.

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中国药物化学杂志
2013年 第3期

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