摘要
目的综述了16元大环内酯类抗生素的作用机制、生物活性及结构修饰等方面的研究现状。方法以近几年国内外有代表性的论文为依据,进行分析、整理和归纳。结果与结论16元大环内酯有显著的抗耐药菌活性,而且具有较低的诱导耐药性。目前已有新的16元大环内酯类药物进入临床研究,有较大的研究空间和开发前景。
关键词
16元大环内酯 /
耐药机制 /
抗菌活性 /
结构修饰
{{custom_keyword}} /
王建强;马淑涛.
16元大环内酯类抗生素的研究进展[J]. 中国药学杂志, 2006, 41(24): 1841-1844
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] HANSEN J L,IPPOLITO J A,BAN N,et al. The structures of four macrolide antibiotics bound to the large ribosomal subunit[J] . Mol Cell,2002,10(1):117-128.
[2] CHAMPNEY W S . Bacterial ribosomal subunit synthesis a novel antibiotic target[J] .Curr Drug Targets Infect Disord,2001,1(1):19-36.
[3] CANU A,MALBRUNY B,COQUEBMONT M,et al. Diversity of ribosomal mutations conferring resistance to macrolides,clindamycin,streptogramin,and telithromycin in Streptococcus pneumoniae[J] . Antimicrob Agents Chemother,2002 ,46(1):125-131.
[4] TAIT-KAMRADT A,DAVIES T,CRONAN M,et al. Mutations in 23S rRNA and ribosomal protein L4 account for resistance in pneumococcal strains selected in vitro by macrolide passage[J] . Antimicrob Agents Chemother,2000 ,44(8):2118-2125.
[5] PEREYRE S,GONZALEZ P,DE BARBEYRAC B,et al. Mutations in 23S rRNA account for intrinsic resistance to macrolides in Mycoplasma hominis and Mycoplasma fermentans and for acquired resistance to macrolides in M. hominis[J] . Antimicrob Agents Chemother,2002,46(10):3142-3150.
[6] ROLAND L,PATRICE C. Resistance to macrolides and related antibiotics in Streptococcus pneumoniae[J] . Antimicrob Agents Chemother,2002,46(9):2727-2734.
[7] DEPARDIEU F,COURVALIN P. Mutation in 23S rRNA responsible for resistance to 16-membered macrolides and streptogramins in Streptococcus pneumoniae[J] .Antimicrob Agents Chemother,2001,45(1):319-323.
[8] FURNERI P M,RAPPAZZO G,MUSUMARRA M P,et al. Two new point mutations at A2062 associated with resistance to 16-membered macrolide antibiotics in mutant strains of Mycoplasma hominis[J] . Antimicrob Agents Chemother,2001,45(10):2958-2960.
[9] SAIER M H. A functional-phylogenetic classification system for transmembrane solute transporters[J] .Microbiol Mol Biol Rev,2000,64(2):354-411.
[10] NILIUS A M,MA Z. Ketolides: the future of the macrolides[J] .Curr Opin Pharmacol,2002,2(5):493-500.
[11] NOBUYOSHI K,KUNIHIKO N,AKIHITO Y. Novel macrolide-specific ABC-type efflux transporter in Escherichia coli[J] .J Bacteriol,2001,183(19):5639-5644.
[12] CLANCY J,DIB-HAJJ F,PETITPAS J W,et al. Cloning and characterization of a novel macrolide efflux gene,mreA,from Streptococcus agalactiae[J] .Antimicrob Agents Chemother,1997,41(12):2719-2723.
[13] KAZUO T,AKIO N,KAZUE T,et al. Identification of functional amino acids in the macrolide 29-phosphotransferase II[J] .Antimicrob Agents Chemother,1999,43(8):2063-2065.
[14] LEONARD K,GARY W A. Translation and protein synthesis: macrolides[J] .Chem Rev,2005,105:499-527.
[15] POULSEN S M,KOFOED C,VESTER B. Inhibition of the ribosomal peptidyl transferase reaction by the mycarose moiety of the antibiotics carbomycin,spiramycin and tylosin[J] . J Mol Biol,2000,304(3):471-481.
[16] MUTAK S,MARSIC N,KRAMARIC M D,et al. Semisynthetic macrolide antibacterials derived from tylosin. Synthesis and structure-activity relationships of novel desmycosin analogues[J] .J Med Chem,2004,47(2):411-431.
[17] PAN L T,JIAN T Y,CHEN Z G,et al. Synthesis and antibacterial activity of a novel class of 4′-substituted 16-membered ring macrolides derived from tylosin[J] .J Med Chem,2004,47(12):2965-2968.
[18] WANG Z,JIAN T,PHAN L T,et al. Synthesis of novel 4′-substituted 16-membered ring macrolide antibiotics derived from leucomycins[J] . Bioorg Med Chem Lett,2004,14(2):519-521.
[19] SHI X G,ZHANG S Q,FAWCETT J P,et al. Acid catalysed degradation of some spiramycin derivatives found in the antibiotic bitespiramycin[J] .J Pharm Biomed Anal,2004,36(3):593-600.
[20] XIANG G S,ZHONG D F,SUN Y M,et al. Metabolites of a novel antibiotic bitespiramycin in rat urine and bile[J] .Chinese Chemical Letters,2004,15(4):431-434.
[21] HONG F U,SAUL M,XIANGRONG G U,et al. Synthesis and in vitro
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}
基金
国家自然科学基金资助项目(20372043)
{{custom_fund}}