CAS: 205110-48-1; Cethromycin

该化合物是一种半合成氯酸酯抗生素,源自红细胞素,旨在将细菌蛋白合成作为目标,与50S血清亚单位结合,它展示了针对抗抗抗大鼠抗菌菌的强力活动,包括抗大鼠菌株,因为它的结合性增强,并减少了对共同抗药机制的易感性.青霉素表明,与早先的大型硫化物相比,其药物遗传特性有所改善,如延长半衰期和更好的组织渗透.它对于呼吸道病原体,包括肺炎和流感嗜血杆菌的广谱效应,使它成为治疗社区肺炎的候选体.在酸性条件下,化合物的稳定性进一步增强了其口腔生物利用率,为抗微生物治疗提供了潜在的临床优势.

结构式图片

上下游产品

acetic acid 2-[4-(5-acetoxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-7-allyloxy-14-ethyl-12,13-dihydroxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yloxy]-4-dimethylamino-6-methyl-tetrahydro-pyran-3-yl ester 2',4-O-diacetyl-6-O-allyl-11,12-cycl°Carbamate erythromycin A acetic acid 2-(11-allyloxy-4-ethyl-8-hydroxy-3a,7,9,11,13,15-hexamethyl-2,6,14-trioxo-tetradecahydro-3,5-dioxa-1-aza-cyclopentacyclotetradecen-10-yloxy)-4-dimethylamino-6-methyl-tetrahydro-pyran-3-yl ester acetic acid 2-(11-allyloxy-4-ethyl-3a,7,9,11,13,15-hexamethyl-2,6,8,14-tetraoxo-tetradecahydro-3,5-dioxa-1-aza-cyclopentacyclotetradecen-10-yloxy)-4-dimethylamino-6-methyl-tetrahydro-pyran-3-yl ester

合成工艺路线路线简述

    📜在 盐酸,甲醇,Ammonium Hydroxide,N-氯代丁二酰亚胺,二甲基硫,Palladium Diacetate,三乙胺,三(邻甲基苯基)磷体系中,用 四氢呋喃,乙醇,二氯甲烷,水,乙腈 用作溶剂,化学反应 312.5H,反应生成喹红霉素
    参考文献:抗菌活性を有する6−o−置換ケトリド
    标题:抗菌活性を有する6−o−置換ケトリド
    摘要:要解决的问题:提供具有抗菌活性的6-O-取代酮烯类化合物,具有酸稳定性,并对革兰氏阴性细菌和大环内酯耐药革兰氏阳性细菌具有增强活性.解决方案:本发明提供6-O-取代红霉素酮烯类衍生物,如式(II)所示,以及包含这些化合物的组合物.[y和z一起形成一个基团x;X是酮基,羟基亚胺基或类似物;或者,Y和z中的一个是h,另一个是氢,羟基或类似物;R是h,羟基;R是h或羟基保护基团;R是取代甲基基团].

    海关参考信息

    专利信息


    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:WO-2024007055-A1
    优先权日:2022-07-05
    标 题 :Method of production of modified phage and method of treatment using same
    发明人:WORMALD PETER-JOHN; VREUGDE SARAH SYLVIA JOSEPH; LIU SHA; PSALTIS ALKIVIADIS JAMES; BOURAS GEORGE SPYRO; SHEARWIN KEITH EDWARD
    权利人:UNIV ADELAIDE; AUSHEALTH CORP PTY LTD
    摘要:A method of producing modified bacteriophage ('phage') that are capable of infecting and causing lysis of a parent host bacteria that is insensitive to the unmodified phage is disclosed. The method comprises: treating a host bacteria insensitive to a selected phage strain with a suitable amount of the said phage strain and at least one antibacterial agent comprising protein synthesis inhibitory activity, and culturing the bacteria for a period and under conditions suitable for the phage to infect the bacteria and replicate to generate progeny phage; and recovering and expanding progeny phage which are phage with a modified capability to infect and cause lysis of said host bacteria. Methods of treatment involving the use of the modified phage, as well as pharmaceutical compositions comprising same are also disclosed.

    专利号:US-12421537-B2
    优先权日:2018-07-06
    标 题:Ribosome variants for sequence defined polymer synthesis
    发明人:JEWETT MICHAEL CHRISTOPHER; D'AQUINO ANNE E
    权利人:UNIV NORTHWESTERN
    摘要:Disclosed are engineered or modified E. coli ribosomes and methods, components, compositions, and kits for preparing and identifying engineered or modified E. coli ribosomes. The engineered or modified E. coli ribosomes may be prepared and identified under a set of defined conditions, such as in the presences of a engineered or modified tRNA comprising a non-natural, non-α-amino acid monomer (NNA), in order to obtain an engineered or modified ribosome that utilizes the engineered or modified tRNA as a substrate for synthesizing a polymer comprising the NNA.

    专利号:US-11382882-B2
    优先权日:2010-03-08
    标 题 :Anti-virulence compositions and methods
    发明人:SHOHAM MENACHEM
    权利人:UNIV CASE WESTERN RESERVE
    摘要:A method of reducing the virulence of a bacterium that expresses accessory gene regulator A (AgrA) includes administering to the bacterium an amount of AgrA antagonist effective to inhibit the synthesis of one or more virulence factors by the bacterium.

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Liang JH. Introduction of a nitrogen-containing side chain appended on C-10 of cethromycin leads to reduced CYP3A4 inhibition (WO2014049356A1). Expert Opin Ther Pat. 2015 Jan;25(1):119-23. doi: 10.1517/13543776.2014.971754. Epub 2014 Oct 18. Review. doi: 10.1345/aph.1R435. Epub 2013 Mar 5. Review. doi: 10.1016/j.ijantimicag.2015.05.001. Epub 2015 Jun 3. doi: 10.1128/AAC.05596-11. Epub 2012 Jan 30.
    5: Wagh B, Paul T, Debrosse C, Klepacki D, Small MC, Mackerell AD Jr, Andrade RB. Desmethyl Macrolides: Synthesis and Evaluation of 4,8,10-Tridesmethyl Cethromycin. ACS Med Chem Lett. 2013 Nov 14;4(11):1114-1118.
    6: Rosenzweig JA, Brackman SM, Kirtley ML, Sha J, Erova TE, Yeager LA, Peterson JW, Xu ZQ, Chopra AK. Cethromycin-mediated protection against the plague pathogen Yersinia pestis in a rat model of infection and comparison with levofloxacin. Antimicrob Agents Chemother. 2011 Nov;55(11):5034-42. doi: 10.1128/AAC.00632-11. Epub 2011 Aug 22.

    合成参考文献


    参考文献:10.1093/jac/48.3.407
    摘要:Weiss K, de Azavedo J, Restieri C, Quach C, Laverdiere M, Rubin E, Gourdeau M, Low DE. In vitro activity of a novel ketolide ABT-773 against invasive strains of Streptococcus pneumoniae. J Antimicrob Chemother. 2001 Sep;48(3):407–9. doi: 10.1093/jac/48.3.407.
    参考文献:10.1093/jac/48.3.447
    摘要:Hunfeld KP, Wichelhaus TA, Kekoukh E, Molitor M, Kraiczy P, Brade V. In vitro susceptibility of the Borrelia burgdorferi sensu lato complex to ABT-773, a novel ketolide. J Antimicrob Chemother. 2001 Sep;48(3):447–9. doi: 10.1093/jac/48.3.447.
    参考文献:10.1128/aac.46.8.2716-2719.2002
    摘要:Finegold SM, Molitoris D, Phan VT, Vaisanen M-, Wexler HM. Activities of ABT-773 against Microaerophilic and Fastidious Organisms. Antimicrob Agents Chemother. 2002 Aug;46(8):2716–9. doi: 10.1128/aac.46.8.2716-2719.2002.
    参考文献:10.1128/aac.00920-05
    摘要:Azoulay-Dupuis E, Mohler J, Bédos JP, Barau C, Fantin B. Efficacy of Cethromycin, a New Ketolide, against Streptococcus pneumoniae Susceptible or Resistant to Erythromycin in a Murine Pneumonia Model. Antimicrob Agents Chemother. 2006 Sep;50(9):3033–8. doi: 10.1128/aac.00920-05.
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