CAS: 74014-51-0; (2S,3S,4R,6S)-6-(((2R,3S,4R,5R,6S)-6-(((4R,5S,6S,7R,9R,10R,11E,13E,16R)-4,10-Dihydroxy-5-Methoxy-9,16-Dimethyl-2-Oxo-7-(2-Oxoethyl)Oxacyclohexadeca-11,13-Dien-6-yl)Oxy)-4-(Dimethylamino)-5-Hydroxy-2-Methyltetrahydro-2H-Pyran-3-yl)Oxy)-2,4-Dimethyl-4-(Propionyloxy)Tetrahydro-2H-Pyran-3-Yl Butyrate

该化合物是一种大型抗生素,其产物是细菌链球菌的发酵所衍生出的大型硅酸抗生素,其特点是大型乳内酯环状结构,这是巨型硅化物的典型特征,具有独特的侧链,有助于其生物活动.罗基他菌具有抗菌特性,特别是针对克菌阳性细菌的抗菌特性,并因其在治疗呼吸道感染和其他细菌疾病方面的效力而闻名.抑制细菌蛋白合成的复合功能,从而阻止细菌的生长和繁殖.除了其抗菌活动外,罗基他菌素还研究其潜在的免疫性循环效应.它的药性肿瘤学包括良好的口服生物利用率和相对较长的半衰期,允许使用方便的剂量疗法.然而,它与其他抗生素一样,可能会产生副作用,如果被滥用,则会导致抗生素的抵抗力.

结构式图片

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    专利信息


    专利号:US-10472663-B2
    优先权日:2015-01-21
    标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
    发明人:FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
    权利人:ABM TECH LLC
    摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

    专利号:WO-9936546-A1
    优先权日:1998-01-14
    标 题 :Polyketides and their synthesis
    发明人:LEADLAY PETER FRANCIS; STAUNTON JAMES; WILKINSON BARRIE; ROWE CHRISTINE JANET; BOHM INES UTE; BUSS ANTONY DAVID
    权利人:GLAXO GROUP LTD; LEADLAY PETER FRANCIS; STAUNTON JAMES; WILKINSON BARRIE; ROWE CHRISTINE JANET; BOHM INES UTE; BUSS ANTONY DAVID
    摘要:The present invention provides an extended polyketide synthase gene assembly comprising a loading module and a plurality of extension modules wherein a second nucleic acid portion, encoding at least one extension module, has been inserted into a first nucleic acid portion encoding the loading module and at least one, and preferably a plurality, of extension modules. Such extended genes are useful in the production of novel macrolides of larger size than the natural product, for example 16-membered ring macrolides instead of 14-membered ring macrolides.

    专利号:ES-2710679-T3
    优先权日:2015-01-21
    标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit the synthesis of proteins

    专利号:US-8933018-B2
    优先权日:2011-02-07
    标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
    发明人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA
    权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC
    摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.

    专利号:EP-3048174-A1
    优先权日:2015-01-21
    标 题:Procedure for the rapid determination of bacterial susceptibilty to antibiotics that inhibit protein synthesis

    专利号:US-2014315720-A1
    优先权日:2012-10-24
    标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
    发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
    权利人:CELANESE ACETATE LLC
    摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
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    主要参考文献


    1: Kim JH, Lee YJ, Sohn HJ, Song KJ, Kwon D, Kwon MH, Im KI, Shin HJ. Therapeutic effect of rokitamycin in vitro and on experimental meningoencephalitis due to Naegleria fowleri. Int J Antimicrob Agents. 2008 Nov;32(5):411-7. doi: 10.1016/j.ijantimicag.2008.05.018. Epub 2008 Aug 30. Epub 2009 Apr 29. doi: 10.1002/jps.22382. Epub 2010 Oct 29. Review. Italian. Japanese.
    11: Fornaseri C, Carbone V, Giangrandi D, Giordano M, Mortellaro C. [Rokitamycin in odontostomatology. Controlled study of doses]. Minerva Stomatol. 1997 Dec;46(12):693-9. Italian. doi: 10.1002/jps.21751. French.

    合成参考文献


    摘要:Chemotherapy, 32(Suppl
    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/s00436-012-3216-z
    摘要:Heredero-Bermejo I, Copa-Patiño JL, Soliveri J, García-Gallego S, Rasines B, Gómez R, de la Mata FJ, Pérez-Serrano J. In vitro evaluation of the effectiveness of new water-stable cationic carbosilane dendrimers against Acanthamoeba castellanii UAH-T17c3 trophozoites. Parasitol Res. 2013 Mar;112(3):961–9. doi: 10.1007/s00436-012-3216-z.
    参考文献:10.2165/00003088-199223020-00004
    摘要:Periti P, Mazzei T, Mini E, Novelli A. Pharmacokinetic drug interactions of macrolides. Clin Pharmacokinet. 1992 Aug;23(2):106–31. doi: 10.2165/00003088-199223020-00004.
    参考文献:10.1016/0378-4347(92)80521-q
    摘要:Tod M, Biarez O, Nicolas P, Petitjean O. Sensitive determination of josamycin and rokitamycin in plasma by high-performance liquid chromatography with fluorescence detection. Journal of Chromatography B: Biomedical Sciences and Applications. 1992 Mar;575(1):171–6. doi: 10.1016/0378-4347(92)80521-q.
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