CAS: 751-97-3; Rolitetracycline

该化合物是一种四环菌类广泛抗生素,具有抑制细菌蛋白合成能力的特征,它源于天然产品氯环环乙烷,并展示了一种与30S 脊椎亚单位结合的类似行动机制,从而防止将氨基乙基-tRNA附于脊椎动物体内,这种抗生素对各种克阳性和克阴性细菌有效,使其有助于治疗各种感染.青石环球素通常通过口服施用,并因其在体内的吸收和分布相对较好而闻名.其化学结构具有环烷核心,具有多羟基和二甲基氨基,有助于其溶性与生物活动.然而,它与其他四环球菌一样,可能会造成副作用,如胃肠扰动和光敏锐等.此外,由于对骨骼和牙齿发育的潜在不利影响,它在某些人群中使用有限,例如孕妇和幼儿.

结构式图片

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CAS号123-75-1 四氢吡咯 | CAS号50-00-0 甲醛

合成工艺路线路线简述

    📜四氢吡咯,聚合甲醛,Alkaline Earth Salt Of/the/ Methylsulfuric Acid 反应生成 罗利环素
    参考文献:Siedel Et Al.,1958,Vol. 100,P. 661
    标题:Siedel Et Al.,1958,Vol. 100,P. 661

    海关参考信息

    专利信息


    专利号:US-9982005-B2
    优先权日:2013-04-04
    标 题 :Macrolides and methods of their preparation and use
    发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
    权利人:HARVARD COLLEGE
    摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

    专利号:US-11466046-B2
    优先权日:2014-10-08
    标题 :14-membered ketolides and methods of their preparation and use
    发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
    权利人:HARVARD COLLEGE
    摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

    专利号:WO-2025128098-A1
    优先权日:2023-12-13
    标 题 :Solid oral dosage forms, kits, and methods of using the same
    发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO
    权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC
    摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).

    专利号:US-9693999-B2
    优先权日:2011-01-26
    标题:Small molecule RNase inhibitors and methods of use
    发明人:DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
    权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
    摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.

    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-2009056955-A1
    优先权日:2007-10-30
    标题 :Amine-bearing phospholipids (abps), their synthesis and use
    发明人:ZUMBUEHL ANDREAS
    权利人:UNIV BASEL; ZUMBUEHL ANDREAS
    摘要:Disclosed herein are amine-bearing phospholipids (ABP). The ABPs display many properties and functionalities of naturally occurring phospholipids, but also new properties and functionalities, such as the ability to polymerize while maintaining structural integrity, that may supplement or expand the functionalities of naturally occurring phospholipids.

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    品牌试剂参考报价(招募中)

    📌 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: Choudhary S, Kishore N. Unraveling the energetics and mode of the recognition of antibiotics tetracycline and rolitetracycline by bovine serum albumin. Chem Biol Drug Des. 2012 Nov;80(5):693-705. doi: 10.1111/cbdd.12009. Epub 2012 Aug 31.
    3: Kobayashi S, Arai S, Hayashi S. In vitro and in vivo effects of combinations of cefotaxime or other beta-lactams with rolitetracycline on methicillin-resistant Staphylococcus aureus. Jpn J Antibiot. 1989 May;42(5):1208-15.

    合成参考文献


    摘要:United States Patent Document., #3846486
    摘要:Drugs in Japan, 6(914), 1982
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