CAS: 35457-80-8; (4R,5S,6S,7R,9R,10R,11E,13E,16R)-6-(((2S,3R,4R,5S,6R)-4-(Dimethylamino)-3-Hydroxy-5-(((2S,4R,5S,6S)-4-Hydroxy-4,6-Dimethyl-5-(Propionyloxy)Tetrahydro-2H-Pyran-2-yl)Oxy)-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-10-Hydroxy-5-Methoxy-9,16-Dimethyl-2-Oxo-7-(2-Ox

该化合物是一种大型滑动抗生素,来自胸膜切除术,主要用于治疗格列阳性病原体和某些克格伦阴性病原体引起的细菌感染,其行动机制包括用与50S 脊髓膜炎分单元捆绑的方法抑制细菌蛋白合成,中子宫颈素显示出对呼吸道感染,皮肤感染和易受感染生物造成的其他条件的功效.一个主要优势是,与其他大型肺炎相比,它相对温和的胃肠道副作用,使它成为对红细胞素或相关抗生素敏感病人的合适选择,还因其在酸性环境中稳定,提高了口腔生物利用率,在肝脏中代谢了中,并主要在薄膜中排出.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

合成工艺路线路线简述

    专利信息


    专利号:US-2022356139-A1
    优先权日:2019-09-03
    标 题:Synthesis of deuterated aldehydes
    发明人:WANG WEI
    权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA
    摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.

    专利号:US-2022395555-A1
    优先权日:2020-06-11
    标题:Derivatives of antibiotics
    发明人:FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH
    权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH
    摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.

    专利号:US-7579167-B2
    优先权日:2002-10-08
    标题:Polypeptides involved in the biosynthesis of spiramycins, nucleotide sequences encoding these polypeptides and applications thereof
    发明人:BLONDELET-ROUAULT MARIE-HELENE; DOMINGUEZ HELENE; DARBON-RONGERE EMMANUELLE; GERBAUD CLAUDE; GONDRAN ANNE; KARRAY FATMA; LACROIX PATRICIA; OESTREICHER-MERMET-BOUVIER NATHALIE; JEAN-LUC PERNODET; TUPHILE KARINE
    权利人:AVENTIS PHARMA S; CENTRE NAT RECH SCIENT
    摘要:The present invention relates to the isolation and identification of novel genes of the biosynthetic pathway for spiramycins and to novel polypeptides involved in this biosynthesis. The invention also relates to a method for producing these polypeptides. It also relates to the use of these genes for the purpose of increasing the levels of production and the purity of the spiramycin produced. The invention relates in particular to a microorganism which produces spiramycin I but which does not produce spiramycin II and III, and to the use of such a microorganism. The invention also relates to the use of the genes of the biosynthetic pathway for spiramycins for constructing mutants which can lead to the synthesis of novel antibiotics or to derived forms of spiramycins. The invention also relates to the molecules produced through the expression of these genes and to pharmacologically active compositions of a molecule produced through the expression of such genes.

    专利号:WO-0112817-A1
    优先权日:1999-08-12
    标题:Evolution and use of enzymes for combinathorial and medicinal chemistry
    发明人:KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    权利人:MAXYGEN INC; LIU LU; KREBBER CLAUS; DAVIS S CHRISTOPHER; DELCARDAYRE STEPHEN; SELIFONOV SERGEY A; HOWARD RUSSELL
    摘要:This invention provides libraries of recombinant derivatizing enzymes that are useful for biocatalytic synthesis of derivatives oforganic molecules, including lead compounds for pharmaceutical use. The recombinant derivatizing enzymes catalyze reactions such as modification or replacement of functional groups on the organicmolecules, or addition of chemical moieties onto preexisting functional groups. The use of recombinant enzyme libraries enables one to obtain enzymes that catalyze the formation of organic molecule derivatives that could not otherwise be made using only naturally occurring enzymes.

    专利号:US-2023399688-A1
    优先权日:2015-08-20
    标 题 :Compositions and multiplexed systems for coupled cell-free transcription-translation and protein synthesis and methods for using them
    发明人:CULLER STEPHANIE; CHEN IHSIUNG BRANDON; PHARKYA PRITI; VAN DIEN STEVE; BARTON NELSON
    权利人:GENOMATICA INC
    摘要:In alternative embodiments, provided herein are transcription/translation (TX-TL) systems and methods of using them for use as rapid prototyping platforms for the synthesis, modification and identification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites, from biosynthetic gene cluster pipelines. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the combinatorial biosynthesis of natural products (NPs), natural product analogs (NPAs) and secondary metabolites. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the rapid prototyping of complex biosynthetic pathways as a way to rapidly assess combinatorial and biosynthetic designs before moving to cellular hosts. In alternative embodiments, these exemplary TX-TL systems are multiplexed for high-throughput (HT) automation and for prototyping engineered platforms for the synthesis or modification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites analogs.

    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.
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    主要参考文献


    1: Zhang X, Li J, Wang C, Song D, Hu C. Identification of impurities in macrolides by liquid chromatography-mass spectrometric detection and prediction of retention times of impurities by constructing quantitative structure-retention relationship (QSRR). J Pharm Biomed Anal. 2017 Oct 25;145:262-272. doi: 10.1016/j.jpba.2017.06.069. Epub 2017 Jul 6. Chinese. doi: 10.4315/0362-028X.JFP-14-100. doi: 10.1159/000358366. Epub 2014 Feb 18. doi: 10.1016/j.biortech.2013.11.073. Epub 2013 Dec 1. doi: 10.1016/j.taap.2013.10.032. Epub 2013 Nov 7. Review. Russian. doi: 10.1016/j.jpba.2013.05.016. Epub 2013 May 20. doi: 10.1016/j.colsurfb.2011.03.037. Epub 2011 Apr 12. Russian. doi: 10.1016/j.janxdis.2010.07.003. Epub 2010 Jul 15. Russian. Chinese. Review. doi: 10.1007/BF02882694. doi: 10.1016/j.jchromb.2007.12.021. Epub 2008 Jan 4. doi: 10.1016/j.bmc.2008.01.027. Epub 2008 Jan 19. Epub 2007 Apr 3.

    合成参考文献


    参考文献:10.7164/antibiotics.33.61
    摘要:Inouye S, Omoto S, Iwamatsu K, Niida T. Modifications of a macrolide antibiotic midecamycin. II. Reaction of midecamycin and 9-acetylmidecamycin with dimethylsulfoxide and acetic anhydride. J Antibiot (Tokyo). 1980 Jan;33(1):61–71. doi: 10.7164/antibiotics.33.61.
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