CAS: 86393-37-5; 6-Fluoro-1-(Methylamino)-7-(4-Methylpiperazin-1-yl)-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

该化合物是一种合成的氟己酮抗生素,其特点是其广泛频谱抗菌活动,主要有效防治各种克模性细菌和克模性细菌,使其在治疗各种感染方面有用; 氨基甲基苯的化学结构包括一个含有氟原子的双环核,这增加了其威力和生物利用率; 展示了一种行动机制,它涉及抑制细菌DNA甘蓝和四角异构体酶IV,对DNA复制和转录至关重要的酶; 氨基丙烯素通常是口服的,以其有利的药用皮肤特性而著称,包括良好的吸收和在组织中的分布; 此外,它与其他抗生素相比,其副作用的发生率相对较低,尽管潜在的不良反应可能包括胃肠扰动,以及在罕见的情况下,对中央...

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上下游产品

CAS号109-01-3 N-甲基哌嗪 | CAS号88569-39-5 4-喹啉甲酸 | CAS号88569-34-0 ethyl 7-chloro-... | CAS号88569-30-6 ethyl 1-amino-7... | CAS号88569-33-9 ethyl 7-chloro-... | CAS号704-10-9 2,4-二氯-5-氟苯乙酮 | CAS号86483-51-4 2,4-二氯-5-氟-Β-氧代苯丙酸乙酯 | CAS号109308-97-6 ethyl 3-N-formy... | CAS号88569-53-3 3-Quinolinecarb...

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  • 88569-33-9 = 86393-37-5 [标题:Reaction Conditions
    标题:Quinolone Compounds
    参考文献:European Patent Organization]

    758-17-8 + 86483-51-4 = 86393-37-5
    反应条件:1.1 -1.2 Solvents: Dichloromethane,Acetic Anhydride2.1 Reagents: Sodium Hydride Solvents: Dimethylformamide3.1 Reagents: Hydrochloric Acid Solvents: Acetonitrile,Water4.1 Solvents: N-Methyl-2-Pyrrolidone
    标题:A Regiospecific Synthesis Of 1-Methylamino-6-Fluoro-7-(4-Methylpiperazin-1-Yl)-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid
    作者:Chu,Daniel T. W.
    参考文献:Journal Of Heterocyclic Chemistry 日期:1985 卷标:22(4) 页码:1033-4]

    704-10-9 = 86393-37-5
    反应条件:1.1 Reagents: Sodium Hydride2.1 -2.2 Solvents: Dichloromethane,Acetic Anhydride3.1 Reagents: Sodium Hydride Solvents: Dimethylformamide4.1 Reagents: Hydrochloric Acid Solvents: Acetonitrile,Water5.1 Solvents: N-Methyl-2-Pyrrolidone
    标题:A Regiospecific Synthesis Of 1-Methylamino-6-Fluoro-7-(4-Methylpiperazin-1-Yl)-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid
    作者:Chu,Daniel T. W.
    参考文献:Journal Of Heterocyclic Chemistry 日期:1985 卷标:22(4) 页码:1033-4]

    109-01-3 = 86393-37-5
    反应条件:1.1 Solvents: Dimethyl Sulfoxide
    标题:Regioselective Nucleophilic Substitution Of Halogen Derivatives Of 1-Substituted 4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acids
    作者:Hermecz,Istvan; Et Al
    参考文献:Heterocycles 日期:1998 卷标:48(6) 页码:1111-1116]

    109-01-3 + 88569-39-5 = 86393-37-5
    反应条件:1.1 Solvents: Dimethyl Sulfoxide
    标题:Regioselective Nucleophilic Substitution Of Halogen Derivatives Of 1-Substituted 4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acids
    作者:Hermecz,Istvan; Et Al
    参考文献:Heterocycles 日期:1998 卷标:48(6) 页码:1111-1116]

    109-01-3 + 88569-39-5 = 86393-37-5
    反应条件:1.1 Solvents: N-Methyl-2-Pyrrolidone
    标题:A Regiospecific Synthesis Of 1-Methylamino-6-Fluoro-7-(4-Methylpiperazin-1-Yl)-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid
    作者:Chu,Daniel T. W.
    参考文献:Journal Of Heterocyclic Chemistry 日期:1985 卷标:22(4) 页码:1033-4]

    109-01-3 + 88569-39-5 = 86393-37-5 [标题:Reaction Conditions
    标题:Quinolone Compounds
    参考文献:European Patent Organization]

    88569-34-0 = 86393-37-5
    反应条件:1.1 Reagents: Hydrochloric Acid Solvents: Acetonitrile,Water2.1 Solvents: N-Methyl-2-Pyrrolidone
    标题:A Regiospecific Synthesis Of 1-Methylamino-6-Fluoro-7-(4-Methylpiperazin-1-Yl)-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid
    作者:Chu,Daniel T. W.
    参考文献:Journal Of Heterocyclic Chemistry 日期:1985 卷标:22(4) 页码:1033-4]

    88569-34-0 = 86393-37-5 [标题:Reaction Conditions
    标题:Quinolone Compounds
    参考文献:European Patent Organization]

    102618-08-6 = 86393-37-5
    反应条件:1.1 Reagents: Sodium Hydride Solvents: Dimethylformamide2.1 Reagents: Hydrochloric Acid Solvents: Acetonitrile,Water3.1 Solvents: N-Methyl-2-Pyrrolidone
    标题:A Regiospecific Synthesis Of 1-Methylamino-6-Fluoro-7-(4-Methylpiperazin-1-Yl)-1,4-Dihydro-4-Oxoquinoline-3-Carboxylic Acid
    作者:Chu,Daniel T. W.
    参考文献:Journal Of Heterocyclic Chemistry 日期:1985 卷标:22(4) 页码:1033-4]

    88569-30-6 = 86393-37-5 [标题:Reaction Conditions
    标题:Quinolone Compounds
    参考文献:European Patent Organization]

    75073-15-3 = 86393-37-5 [标题:Reaction Conditions
    标题:Quinolone Compounds
    参考文献:European Patent Organization
📜7-氯-6-氟-4-氧代-1,4-二氢喹啉-3-羧酸乙酯置于sodium Hydroxide,乙酸酐,Potassium Carbonate,2,4-二硝基苯基羟胺体系中,用 吡啶,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 22.0H,反应生成 氨氟沙星
参考文献:Novel Amino-Substituted 3-Quinolinecarboxylic Acid Antibacterial Agents: Synthesis And Structure-Activity Relationships
标题:Novel Amino-Substituted 3-Quinolinecarboxylic Acid Antibacterial Agents: Synthesis And Structure-Activity Relationships
摘要:A Series Of Novel 3-Quinolinecarboxylic Acid Derivatives Have Been Prepared And Their Antibacterial Activity Evaluated. These Derivatives Are Characterized By Fluorine Attached To The 6-Position And Substituted Amino Groups Appended To The 1-And 7-Positions. Structure-Activity Relationship Studies Indicate That Antibacterial Potency Is Greatest When The 1-Substituent Is Methylamino And The 7-Substituent Is Either 4-Methyl-1-Piperazinyl,16,Or 1-Piperazinyl,21. Derivatives 16 And 21,The 1-Methylamino Analogues Of Pefloxacin And Norfloxacin,Respectively,Show Comparable In Vitro And In Vivo Antibacterial Potency To These Two Known Agents. The Activity (Vs. Escherichia Coli Vogel) Of 16 (Amifloxacin) Is The Following: In Vitro Mic (Microgram/ml) = 0.25; In Vivo (Mice) Pd50 (Mg/kg) = 1.0 (Po),0.6 (Sc).
DOI:10.1021/jm00375A003

海关参考信息

专利信息


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-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-2009054643-A1
优先权日:2007-05-24
标 题:Novel method of synthesis of fluoroquinolones

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.

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主要参考文献


1: Venezia RA, Prymas LA, Shayegani A, Yocum DM. In vitro activities of amifloxacin and two of its metabolites. Antimicrob Agents Chemother. 1989 May;33(5):762-6.
2: Iravani A, Welty GS, Newton BR, Richard GA. Effects of changes in pH, medium, and inoculum size on the in vitro activity of amifloxacin against urinary isolates of Staphylococcus saprophyticus and Escherichia coli. Antimicrob Agents Chemother. 1985 Apr;27(4):449-51.

合成参考文献


参考文献:10.1021/jm030986y
摘要:Cianchetta G, Mannhold R, Cruciani G, Baroni M, Cecchetti V. Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach. J Med Chem. 2004 Jun 03;47(12):3193–201. doi: 10.1021/jm030986y.
参考文献:10.1021/jm00153a015
摘要:Domagala JM, Hanna LD, Heifetz CL, Hutt MP, Mich TF, Sanchez JP, Solomon M. New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay. J Med Chem. 1986 Mar;29(3):394–404. doi: 10.1021/jm00153a015.
参考文献:10.1021/jm00154a003
摘要:Domagala JM, Heifetz CL, Mich TF, Nichols JB. 1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity. J Med Chem. 1986 Apr;29(4):445–8. doi: 10.1021/jm00154a003.
参考文献:10.1007/bf02013968
摘要:Høiby N. Clinical uses of nalidixic acid analogues: the fluoroquinolones. European Journal of Clinical Microbiology & Infectious Diseases. 1986 Apr;5(2):138–40. doi: 10.1007/bf02013968.
参考文献:10.1016/0163-7258(85)90005-1
摘要:Diana GD, Otto MJ, McKinlay MA. Inhibitors of picornavirus uncoating as antiviral agents. Pharmacology & Therapeutics. 1985 Jan;29(3):287–97. doi: 10.1016/0163-7258(85)90005-1.
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