CAS: 108319-06-8; 1-(2,4-Difluorophenyl)-6-Fluoro-7-(3-Methylpiperazin-1-yl)-4-Oxoquinoline-3-Carboxylic Acid

该化合物是一种氟己酮抗生素,其抗药性广泛,针对克己阳性和克己氨基细菌,其行动机制包括抑制细菌DNA gyraase 和TOP异构体IV,干扰DNA复制和转录;Temafloxain展示了对呼吸病原体,包括肺炎和流感嗜血杆菌的抗药性,以及针对Legionella和Mycoplasma等非典型生物体的活动.该化合物展示了有利的药效活性,口服生物利用率和组织渗透率良好,特别是在肺部,其平衡的频谱和药性特征使它成为治疗呼吸道和尿道感染的候选体.然而,临床使用由于安全考虑而停止,尽管它仍然对抗微生物研究感兴趣.

结构式图片

上下游产品

Ethyl 1-(2,4-Difluorophenyl)-6,7-Difluoro-1,4-Dihydro-4-Oxoquinoline-3-Carboxylate 108138-17-6

合成工艺路线路线简述

    📜Ethyl 1-(2,4-Difluorophenyl)-6,7-Difluoro-1,4-Dihydro-4-Oxoquinoline-3-Carboxylate,2-甲基哌嗪,Sodium Hydroxide 以64%的收率获得
    参考文献:Narita Hirokazu; Konishi Yoshinori; Nitta Jun; Nagaki Hideyoshi; Kobayash+,J. Pharm. Soc. Jap.,106,(1986) N 9,795-801
    标题:Narita Hirokazu; Konishi Yoshinori; Nitta Jun; Nagaki Hideyoshi; Kobayash+,J. Pharm. Soc. Jap.,106,(1986) N 9,795-801

    海关参考信息

    专利信息


    专利号:US-2024197774-A1
    优先权日:2021-04-16
    标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
    发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
    权利人:UNIV TEXAS
    摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

    专利号:US-11332444-B2
    优先权日:2018-04-25
    标题:Method for the hydrolysis of quinolonecarboxylic esters
    发明人:FEY PETER; BERWE MATHIAS; WIRTHS Joerg; WISCHNAT RALF; LONGERICH MARKUS; DIETZEL ANTJE
    权利人:BAYER ANIMAL HEALTH GMBH
    摘要:Quinolonecarboxylic esters of the general formula (II) are hydrolyzed to quinolonecarboxylic acids of the general formula (I):The method comprises the step A):A) reacting compounds of the formula (II) with a mixture comprising acetic acid, sulfuric acid and waterIn step A), ≥30 to ≤40 mol of acetic acid, ≥0.3 to ≤1 mol of sulfuric acid and ≥0.9 to ≤2.5 mol of water are used per mole of compounds of the formula (II). The method is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin.

    专利号:US-8093381-B2
    优先权日:2007-05-24
    标题:Method of synthesis of fluoroquinolones
    发明人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS
    权利人:BERTHON-CEDILLE LAURENCE; LEGUERN MARIE-EMMANUELLE; RENAUD GILLES; TOMBRET FRANCIS; BIOCODEX
    摘要:The invention relates to a method of preparation of fluoroquinolones of formula (I) from compounds of formula (II): n nin which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and X are as defined in Claim 1.

    专利号:US-10443047-B2
    优先权日:2014-05-01
    标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
    发明人:TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
    权利人:NOVOGY INC
    摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

    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-8399502-B2
    优先权日:2008-09-17
    标 题 :Analogs of indole-3-carbinol and their use as agents against infection
    发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
    权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
    摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

    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: Owens RC Jr, Ambrose PG. Antimicrobial safety: focus on fluoroquinolones. Clin Infect Dis. 2005 Jul 15;41 Suppl
    2:S144-57. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Review. Russian. Review. Review. Review. Review. Review. Review. Review. Review.

    合成参考文献


    参考文献:10.1007/bf01849631
    摘要:Csemiczky G, Alvendal C, Landgren BM. Risk for ovulation in women taking a low-dose oral contraceptive (Microgynon) when receiving antibacterial treatment with a fluoroquinolone (ofloxacin). Adv Contracept. 1996 Jun;12(2):101–9. doi: 10.1007/bf01849631.
    参考文献:10.1007/bf00900953
    摘要:Pastor P, Moitinho E, Elizalde I, Cirera I, Tolosa E. Reversible oral-facial dyskinesia in a patient receiving ciprofloxacin hydrochloride. J Neurol. 1996 Aug;243(8):616–7. doi: 10.1007/bf00900953.
    参考文献:10.2165/00003495-199652030-00006
    摘要:Bryson HM, Spencer CM. Quinupristin-dalfopristin. Drugs. 1996 Sep;52(3):406–15. doi: 10.2165/00003495-199652030-00006.
    参考文献:10.2165/00003088-199630030-00003
    摘要:Pichini S, Altieri I, Zuccaro P, Pacifici R. Drug monitoring in nonconventional biological fluids and matrices. Clin Pharmacokinet. 1996 Mar;30(3):211–28. doi: 10.2165/00003088-199630030-00003.
    参考文献:10.2165/00003495-199957060-00002
    摘要:Momméja-Marin H, Carbon C. What is the place of fluoroquinolones in the treatment of community-acquired respiratory tract infections Drugs. 1999 Jun;57(6):851–3. doi: 10.2165/00003495-199957060-00002.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知