CAS: 153808-85-6; (S)-1-Cyclopropyl-8-(Difluoromethoxy)-6-Fluoro-7-(3-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丁阳性和克丁丁菌,有助于治疗各种感染;该化合物具有典型的氟丙酮的双环核心结构,包括氟丙酮原子,可增强抗菌能;卡德罗弗罗克辛通过抑制细菌DNA甘蓝酶和对DNA复制和转录至关重要的异构酶IV,抑制了对DNA复制和转录至关重要的酶IV;这一机制扰乱了细菌细胞的分化和生长;该物质一般以口服形式施用,以其有利的药用植物特性为人知,包括良好的吸收和组织中的分布;但与其他抗生素一样,它可能会产生副作用,包括胃肠扰动和对中...

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    专利信息


    专利号:US-2025170267-A1
    优先权日:2022-02-28
    标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof
    发明人:TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO
    权利人:UBE CORP
    摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).

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    主要参考文献


    1: Masuda N, Takahashi Y, Otsuki M, Ibuki E, Miyoshi H, Nishino T. In vitro and in vivo antibacterial activities of CS-940, a new 6-fluoro-8-difluoromethoxy quinolone. Antimicrob Agents Chemother. 1996 May;40(5):1201-7. doi: 10.1128/AAC.40.5.1201.
    2: Biedenbach DJ, Sutton LD, Jones RN. Antimicrobial activity of CS-940, a new trifluorinated quinolone. Antimicrob Agents Chemother. 1995 Oct;39(10):2325-30. doi: 10.1128/AAC.39.10.2325.
    3: Schmitz FJ, Jones ME. Antibiotics for treatment of infections caused by MRSA and elimination of MRSA carriage. What are the choices? Int J Antimicrob Agents. 1997 Jun;9(1):1-19. doi: 10.1016/s0924-8579(97)00027-7. 41(11):2582-5. doi: 10.1128/AAC.41.11.2582.

    合成参考文献


    摘要:Yamane N, Chilima BZ, Tosaka M, Okazawa Y, Tanno K. [Determination of antimycobacterial activities of fluoroquinolones against clinical isolates of Mycobacterium tuberculosis: comparative determination with egg-based Ogawa and agar-based Middlebrook 7H10 media]. Kekkaku. 1996 Aug;71(8):453–8.
    摘要:Tanimura H, Ohnishi H. [Transfer of cadrofloxacin, a novel fluoroquinolone antibacterial, into the gallbladder tissue and bile]. Jpn J Antibiot. 2004 Feb;57(1):118–23.
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