108319-06-8

• 常用中文名：替马沙星
• 常用英文名：temafloxacin
• CAS号：108319-06-8
• 分子式：C₂₁H₁₈F₃N₃O₃
• 分子量：417.38100
• 相关类别： 原料药 人工合成抗感染类药 喹诺酮类药
• 发布时间：2018-07-27 18:46:34
• 更新时间：2024-01-09 12:45:01
• 替马沙星(TMFX)是一种喹诺酮类抗菌剂,对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有广泛的抗菌谱[1][2]。

名称

• 中文名: 替马沙星
• 英文名: 1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid
• 中文别名: 1-(2,4-二氟苯基)-6-氟-1,4-二氢-7-(3-甲基-1-哌嗪基)-4-氧-3-喹啉羧酸
• 英文别名: [14C]-Temafloxacin; Temafloxacina [Spanish]; 1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid; Temafloxacina; 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-7-(3-methyl-1-piperazinyl)-quinoline-3-carboxylic acid; Omniflox; Temafloxacinum [Latin]; Temafloxacine; 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxoquinoline-3-carboxylic acid; Temafloxacinum; Temafloxacine [French]; Temafloxacin

物化性质

• 密度: 1.427g/cm3
• 沸点: 608.9ºC at 760mmHg
• 分子式: C₂₁H₁₈F₃N₃O₃
• 分子量: 417.38100
• 闪点: 322.1ºC
• 精确质量: 417.13000
• PSA: 74.57000
• LogP: 3.29810
• 蒸汽压: 1.11E-15mmHg at 25°C
• 折射率: 1.603
• 储存条件: 2-8°C

生物活性

• 描述: 替马沙星(TMFX)是一种喹诺酮类抗菌剂,对革兰氏阳性菌、革兰氏阴性菌和厌氧菌具有广泛的抗菌谱[1][2]。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
• 体外研究: 替莫沙星对革兰氏阳性菌和革兰氏阴性菌具有广泛的抗菌活性,包括对肺炎链球菌、人型支原体和厌氧菌(包括脆弱类杆菌)的体外抗菌活性提高[2]。
• 体内研究: 替马沙星是一种氟喹诺酮类药物,半衰期为7-8小时,胃肠道吸收迅速。除中枢神经系统(CNS)外,替莫沙星具有良好的组织和体液渗透性和浓度[2]。
• 参考文献:

  [1]. S Matsuda, et al. Experimental and clinical studies of temafloxacin in the field of obstetrics and gynecology. Jpn J Antibiot. 1993 Jun;46(6):492-504.

  [2]. G A Pankey. Temafloxacin: an overview. Am J Med. 1991 Dec 30;91(6A):166S-172S.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : VB1999065 CHEMICAL NAME : 3-Quinolinecarboxylic acid, 1,4-dihydro-1-(2,4-difluorophenyl)-6-fluoro-7- (3-methyl-1-piperazinyl)-4-oxo- CAS REGISTRY NUMBER : 108319-06-8 LAST UPDATED : 199612 DATA ITEMS CITED : 6 MOLECULAR FORMULA : C21-H18-F3-N3-O3 MOLECULAR WEIGHT : 417.42 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 36400 mg/kg/26W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain Nutritional and Gross Metabolic - changes in sodium TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 18200 mg/kg/26W-I TOXIC EFFECTS : Cardiac - EKG changes not diagnostic of specified effects Musculoskeletal - joints Nutritional and Gross Metabolic - weight loss or decreased weight gain MUTATION DATA TYPE OF TEST : DNA repair TEST SYSTEM : Bacteria - Bacillus subtilis DOSE/DURATION : 20 mg/L REFERENCE : AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 37,213,1993