CAS: 105956-99-8; 7-(3-Aminopyrrolidin-1-yl)-8-Chloro-1-Cyclopropyl-6-Fluoro-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid Hydrochloride

该化合物是一种合成的五氟丙酮抗生素,其特点是其广泛频谱抗菌活动,主要有效防治各种克型阳性细菌和克型阴性细菌,使其在治疗各种感染方面有用;该化合物具有典型的氟丙酮的双环核心结构,包括增强抗菌能的氟丙酮原子;盐酸丙烯丙烯丙烯酯在水中溶解,有利于其在临床环境中的行政管理;其行动机制包括抑制细菌DNA甘蓝酶和对DNA复制和修复至关重要的异构酶IV,这种抗生素经常用于治疗呼吸道和尿道感染以及皮肤和软组织感染;然而,与其他氟丙酮一样,它可能与潜在的副作用有关,包括胃肠扰动,在稀有的情况下,也与局部损害有关;对于任何抗生素而言,适当使用对于减轻抗生素抗药性的风险至关重要.

结构式图片

合成工艺路线路线简述

    📜8-氯-1-环丙基-6,7-二氟-1,4-二氢-4-氧代-3-喹啉羧酸,3-(Boc-氨基)吡咯烷,乙腈,三乙胺,盐酸,溶剂黄146 以84%的收率获得
    参考文献:Sanchez,Joseph P.;Domagala,John M.;Hagen,Susan E.;Heifetz,Carl L.;Hut+,J. Med. Chem.,31,(1988) N 5,983-991
    标题:Sanchez,Joseph P.;Domagala,John M.;Hagen,Susan E.;Heifetz,Carl L.;Hut+,J. Med. Chem.,31,(1988) N 5,983-991

    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-9907753-B2
    优先权日:2010-03-19
    标 题 :Lipid vesicle compositions and methods of use
    发明人:IRVINE DARRELL J; MOON JAEHYUN
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:The invention provides delivery systems comprised of stabilized multilamellar vesicles, as well as compositions, methods of synthesis, and methods of use thereof. The stabilized multilamellar vesicles may comprise prophylactic, therapeutic and/or diagnostic agents.

    专利号:US-6911318-B2
    优先权日:1999-03-03
    标 题:Bacterial transglycosylases: assays for monitoring the activity using Lipid II substrate analogs and methods for discovering new antibiotics
    发明人:KAHNE SUZANNE WALKER
    权利人:UNIV PRINCETON
    摘要:This invention provides a direct method for monitoring bacterial transglycosylase activity using labeled substrates produced by chemo-enzymatic synthesis wherein the labels are selected to permit the detection of both polymeric and non-polymeric products simultaneously, either directly or following the separation of product from starting material. The invention promotes the discovery of new antibiotics with activity against bacterial transglycosylases by a) laying the groundwork for structural analysis of purified, active transglycosylase (which permits structure-based design); and b) providing an assay that can be used to screen for inhibitors.

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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: Majalekar PP, Shirote PJ. Fluoroquinolones: Blessings Or Curses. Curr Drug Targets. 2020;21(13):1354-1370. doi: 10.2174/1389450121666200621193355. 29(4):378-80. doi: 10.1177/106002809502900407. 45(9):2543-52. doi: 10.1128/AAC.45.9.2543-2552.2001.
    4: Siami FS, LaFleur BJ, Siami GA. Clinafloxacin versus piperacillin/tazobactam in the treatment of severe skin and soft-tissue infections in adults at a Veterans Affairs medical center. Clin Ther. 2002 Jan;24(1):59-72. doi: 10.1016/s0149-2918(02)85005-6. 27(3):166-72. doi: 10.1007/BF02561522. Severe Skin and Soft Tissue Infections Study Group. Clinafloxacin versus piperacillin-tazobactam in treatment of patients with severe skin and soft tissue infections. Antimicrob Agents Chemother. 2001 Feb;45(2):525-31. doi: 10.1128/AAC.45.2.525-531.2001.
    7: Randinitis EJ, Koup JR, Rausch G, Abel R, Bron NJ, Hounslow NJ, Vassos AB, Sedman AJ. Clinafloxacin pharmacokinetics in subjects with various degrees of renal function. Antimicrob Agents Chemother. 2001 Sep;45(9):2536-42. doi: 10.1128/AAC.45.9.2536-2542.2001.

    合成参考文献


    参考文献:10.1007/s150100070018
    摘要:Oh H, Nord CE, Barkholt L, Hedberg M, Edlund C. Ecological disturbances in intestinal microflora caused by clinafloxacin, an extended-spectrum quinolone. Infection. 2000 Sep;28(5):272–7. doi: 10.1007/s150100070018.
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