CAS: 167887-97-0; (S)-5-Amino-7-(7-Amino-5-Azaspiro[2.4]Heptan-5-yl)-1-Cyclopropyl-6-Fluoro-8-Methyl-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid
该化合物是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己体和克己体细菌,使其在治疗各种感染方面有用;该化合物具有典型的氟己醇的双环核心结构,其中包括氟己体原子,可增强抗菌剂的能耐力;Olamufloxinacin通过抑制细菌DNAgyraase 和topo 异构体酶IV(对DNA复制和转录至关重要的酶)而开展的工作;这一行动机制导致细菌细胞分解的中断,最终导致细胞死亡;该物质通常以口头方式施用,并因其有利的致癌特性而为人所知,包括良好的吸收和组织内的分布;此外,与其他抗药性相比,其副作用的发生率相对较低,但抗药性会发展得不适当;与所有抗生素一样,必须明智地使用Olamufloxinacin,以尽量减少抗药性风险,并确保其在临床环境中继续有效.
- 英文名称(S)-5-Amino-7-(7-Amino-5-Azaspiro[2.4]Heptan-5-yl)-1-Cyclopropyl-6-Fluoro-8-Methyl-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid
- 中文名称欧拉沙星
- IUPAC名称(S)-5-amino-7-(7-amino-5-azaspiro[2.4]heptan-5-yl)-1-cyclopropyl-6-fluoro-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
- 其它别名5-Amino-7-((S)-7-Amino-5-Azaspiro[2.4]Hept-5-yl)-1-Cyclopropyl-6-Fluoro-1,4-Dihydro-8-Methyl-4-Oxoquinoline-3-Carboxylic Acid; 3-Quinolinecarboxylic Acid, 5-Amino-7-[(7S)-7-Amino-5-Azaspiro[2.4]Hept-5-Yl]-1-Cyclopropyl-6-Fluoro-1,4-Dihydro-8
- CAS编号167887-97-0
- MFCD编号:MFCD00938243
- FDA UNII编号:LJG8KL1435
- 分子式:C20H23FN4O3分子量:386.43
- 产品CID: 848870
- 产品分类原料药 → 人工合成抗感染类药 → 喹诺酮类药
物理性质
MSDS等安全信息
上下游产品
5-amino-7-((S)-7-tert-butoxycarbonylamino-5-azaspiro[2.4]hept-5-yl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid (7S)-5-azaspiro[2.4]heptan-7-ylcarbamic acid tert-butyl ester 5-amino-1-cyclopropyl-6,7-difluoro-8-methyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid 5-acetylamino-7-[(7S)-7-tert-butoxycarbonylamino-5-azaspiro[2.4]hept-5-yl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methyl-4-oxoquinoline-3-carboxylic acid合成工艺路线路线简述
海关参考信息
- 2902300000-甲苯
2905110000-甲醇
2912110000-甲醛
2915110000-甲酸 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
- 详情请参考：📖 海关编码查询和海关进出口税则
专利信息
专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.
专利号:CA-2551859-C
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
专利号:EP-2250143-A2
优先权日:2008-01-25
标题 :Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
专利号:WO-2005066122-A2
优先权日:2003-12-30
标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
专利号:EP-2250143-B1
优先权日:2008-01-25
标 题 :Method for the enzymatic kinetic resolution of acyloxyalkyl thiocarbonates used for the synthesis of acyloxyalkyl carbamates
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
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主要参考文献
1: Sun J, Deguchi Y, Tauchi Y, He Z, Cheng G, Morimoto K. Distribution characteristics of orally administered olamufloxacin, a newly synthesized fluoroquinolone antibacterial, in lung epithelial lining fluid and alveolar macrophage in rats. Eur J Pharm Biopharm. 2006 Oct;64(2):238-45. Epub 2006 Jun 23. Review. Epub 2003 Nov 12. doi: 10.1002/chem.201702362. Epub 2017 Oct 10. Review. Epub 2004 Dec 8.
10: Yoshizumi S, Domon H, Miyazaki S, Yamaguchi K. In vivo activity of HSR-903, a new fluoroquinolone, against respiratory pathogens. Antimicrob Agents Chemother. 1998 Apr;42(4):785-8.
11: Frean J, Klugman KP, Arntzen L, Bukofzer S. Susceptibility of Yersinia pestis to novel and conventional antimicrobial agents. J Antimicrob Chemother. 2003 Aug;52(2):294-6. Epub 2003 Jul 15.
合成参考文献
参考文献:10.1093/jac/dkh001
摘要:Higa F, Arakaki N, Tateyama M, Koide M, Shinzato T, Kawakami K, Saito A. In vitro and in vivo activity of olamufloxacin (HSR-903) against Legionella spp. J Antimicrob Chemother. 2003 Dec;52(6):920–4. doi: 10.1093/jac/dkh001.
参考文献:10.1093/jac/40.3.437
摘要:Deguchi T, Yasuda M, Ishihara S, Takahashi Y, Okezaki E, Nagata O, Saito I, Kawada Y. In-vitro antimicrobial activity of HSR-903, a new fluoroquinolone, against clinical isolates of Neisseria gonorrhoeae with quinolone resistance-associated alterations in GyrA and ParC. J Antimicrob Chemother. 1997 Sep;40(3):437–9. doi: 10.1093/jac/40.3.437.
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