CAS: 32887-01-7; (2S,5R,6R)-6-(((E)-Azepan-1-Ylmethylene)Amino)-3,3-Dimethyl-7-Oxo-4-Thia-1-Azabicyclo[3.2.0]Heptane-2-Carboxylic Acid

该化合物是一种属于青霉素类的乙酯抗生素,专门设计用于锁定和抑制细菌细胞壁合成,对某些克格朗阴性细菌,包括大肠杆菌和蛋白甲虫菌菌株特别有效. 鼠胆碱酯酶对含有青霉素的蛋白质(PBPs)具有约束作用,对细菌细胞壁中小狗类层的交叉连接至关重要,最终导致细胞分解和死亡. 这种抗生素的特点是对人类细胞的毒性相对较低,使它成为治疗尿道感染和其他细菌感染的合适选择. 麻疹经常通过口服口服,并因其稳定性而为人所知,尽管它可能对其他人有影响. 它的药理遗传特性包括体内的很好的吸收和分布,而肾外泄是主要消除途径.

结构式图片

上下游产品

CAS号551-16-6 6-氨基青霉烷酸 | CAS号65009-95-2 hexahydro-1-(me...

合成工艺路线路线简述

    📜6-氨基青霉烷酸,六氢-1-(甲氧基亚甲基)-1H-氮杂卓鎓硫酸甲酯盐置于三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应生成 美西林
    参考文献:Studies On Prodrugs. Vi Preparation And Characterization Of (5-Substituted 2-Oxo-1,3-Dioxol-4-yl)Methyl Esters Of Mecillinam.
    标题:Studies On Prodrugs. Vi Preparation And Characterization Of (5-Substituted 2-Oxo-1,3-Dioxol-4-yl)Methyl Esters Of Mecillinam.
    摘要:作为一种新型甲氧西林原药,我们制备了甲氧西林(5-取代的 2-氧代-1,3-二氧戊环-4-基)甲酯.研究发现,小鼠口服这些酯类药物后,血液中的美西林含量至少是美西林本身的 4 倍.美西林(5-甲基-2-氧代-1,3-二氧戊环-4-基)甲酯盐酸盐具有吸湿性,但其 L-酒石酸盐不具有吸湿性.
    DOI:10.1248/cpb.35.642

    海关参考信息

    专利信息


    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: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.

    专利号:US-9868747-B2
    优先权日:2014-02-18
    标题:Marinopyrrole derivatives and methods of making and using same
    发明人:LI RONGSHI; SEBTI SAID; LIU YAN; QIN YONG; SONG HAO; CHENG CHUNWEI
    权利人:H LEE MOFFITT CANCER CT & RES; CHONGQING ZEIN PHARMACEUTICAL CO LTD
    摘要:Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.

    专利号:US-2025002508-A1
    优先权日:2020-05-05
    标题 :Boronic acid derivatives and synthesis, polymorphic forms, and therapeutic uses thereof
    发明人:HECKER SCOTT J; BOYER SERGE HENRI; BIO MATTHEW M; FANG YUANQING; GONZALES DE CASTRO ANGELA; LEFORT LAURENT; ZHU ZUOLIN; LINDER THOMAS
    权利人:QPEX BIOPHARMA INC
    摘要:Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

    专利号:CN-109371095-A
    优先权日:2018-12-06
    标题 :A kind of method of enzymatic synthesis of amoxicillin

    专利号:US-4452796-A
    优先权日:1982-06-14
    标题:6-Aminoalkylpenicillanic acid 1,1-dioxides as beta-lactamase inhibitors
    发明人:BARTH WAYNE E
    权利人:PFIZER
    摘要:Beta-lactamase inhibitors which are 6-alpha- and 6-beta-(aminomethyl) and (1-aminoethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, used in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoalkyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also used in the treatment of bacterial infections; and intermediates therefor.

    供应商参考报价(招募中)

    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: Farrar WE. Amdinocillin. Ann Intern Med. 1984 Sep;101(3):389-90. doi: 10.7326/0003-4819-101-3-389. 5(1):1-10. doi: 10.1002/j.1875-9114.1985.tb04448.x. 75(2A):48-53. doi: 10.1016/0002-9343(83)90093-1. 75(2A):72-81. doi: 10.1016/0002-9343(83)90098-0. 59(3):1718-27. doi: 10.1128/AAC.04819-14. Epub 2015 Jan 12.
    6: Amdinocillin. Med Lett Drugs Ther. 1985 Mar 29;27(684):30-2. 75(2A):9-20. doi: 10.1016/0002-9343(83)90089-x. 75(2A):113-8. doi: 10.1016/0002-9343(83)90105-5. 75(2A):85-9. doi: 10.1016/0002-9343(83)90100-6. 159(6):1065-72. doi: 10.1093/infdis/159.6.1065. 75(2A):100-5. doi: 10.1016/0002-9343(83)90103-1. 75(2A):30-41. doi: 10.1016/0002-9343(83)90091-8. 1(8058):252-3. 1(7984):503-5. 75(2A):54-9. doi: 10.1016/0002-9343(83)90094-3. 75(2A):119-24. doi: 10.1016/0002-9343(83)90106-7. 159(6):1300-11. doi: 10.1016/j.cell.2014.11.017.
    18: Freyhult E, Bremell D, Tängden T. Pivmecillinam – ett osäkert alternativ vid pyelonefrit. Lakartidningen. 2020 Aug 21;117:20048. Swedish. 32(11):1632-5. doi: 10.1128/AAC.32.11.1632.

    合成参考文献


    参考文献:10.1046/j.1469-0691.2002.00376.x
    摘要:Bruun B, Gahrn-Hansen B. Mecillinam susceptibility as an indicator of beta-lactamase production in Staphylococcus aureus. Clin Microbiol Infect. 2002 Feb;8(2):122–4. doi: 10.1046/j.1469-0691.2002.00376.x.
    参考文献:10.1093/jac/dkh233
    摘要:Bostock JM, Geary I, Eley A, Chopra I. Mecillinam has potent in vitro activity against Chlamydophila pneumoniae ATCC VR1310. J Antimicrob Chemother. 2004 Jun;53(6):1112. doi: 10.1093/jac/dkh233.
    参考文献:10.1007/978-1-4939-2854-5_1
    摘要:Verstraeten N, Knapen W, Fauvart M, Michiels J. A Historical Perspective on Bacterial Persistence. Methods Mol Biol. 2016;1333():3–13. doi: 10.1007/978-1-4939-2854-5_1.
    参考文献:10.1016/j.ijantimicag.2016.11.021
    摘要:Zayyad H, Eliakim-Raz N, Leibovici L, Paul M. Revival of old antibiotics: needs, the state of evidence and expectations. International Journal of Antimicrobial Agents. 2017 May;49(5):536–41. doi: 10.1016/j.ijantimicag.2016.11.021.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知