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喹诺酮类抗菌药物的合成研究进展 被引量：1

Progress in the Synthesis of Quinolones as Antibacterial Agents
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摘要 喹诺酮类抗菌药物是一类全合成的活性化合物,具有抗菌谱广、作用机制独特、高效低毒等特点,其发展已历经4代。综述喹诺酮类化合物的骨架合成方法及结构修饰研究的最新进展,简要介绍其中代表性化合物的抗菌活性及构效关系。 Quinolones are among the total synthetic antibacterial compounds characterized by broad spectrum, unique mechanism of action, high activity and low toxicity, of which the development has experienced four generations. The recent progress in the approach to synthesize 4-quinolone skeleton and the structural modification of quinolones as antibacterial agents was reviewed. The antibacterial activity and structure-activity relationship of the representative compounds were briefly introduced.
作者 唐琰 丁雁 刘嵘 朱雄
机构地区 中国药科大学医药化工研究所
出处 《药学进展》 CAS 2012年第10期433-444,共12页 Progress in Pharmaceutical Sciences
基金 江苏省教育厅高校科研成果产业化推进工程项目(No.JH09-29)
关键词 喹诺酮 合成 结构修饰 抗菌活性 构效关系 quinolone synthesis structural modification antibacterial activity structure-activity rela- tionship
分类号 R914 [医药卫生—药物化学]
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  • 9Synthesis of l-cyclopropyl-6-fluoro-7-(3-aminopyrrolo[3,4-c] pyrazol-5(2H,4H,6H)-yl)-1,4-dihydro-4-oxo-1,8-naphthy-ridine-3-carboxylic acid (6a):a mixture of 2 (0.38 g,1.9 mmol),5 (0.53 g,1.3 mmol),triethylamine (1.0 mL) and anhydrous acetonitrile (10 mL) was stirred at room temperature for 0.5 h,and then concentrated in vacuo.To the residue was added 5% NaOH solution (6.0 mL),the reaction mixture was stirred at 40 ℃ for 0.5 h and then adjusted to pH 5 with 2 mol/L HCI.The precipitate was collected by suction to give off-white amorphous product 6a (0.32 g,66.5%).
  • 10Typicaldataofthe syntheticcompounds:6f1HNMR(400 MHz,DMSO-d6):δ 1.00-1.18 (m,4H),4.05-4.09 (m,IH),4.57-4.60(m,4H),6.88 (t,1H),8.63 (s,1H),7.87 (d,1H),8.75 (s,1H); 13C NMR (400 MHz,DMSO-d6):δ 9.3,40.8,49.5,49.8,107.2,108.8,109.1,114.7,117.3,118.2,119.9,130.7,135.4,142.2,151.2,152.4,154.9,165.3,175.7; HRMS-ESI m/z:458.10554(calcd.for C19H16F3N5O4Na,458.10521[M+Na] +).7f 1H NMR (400 MHz,DMSO-d6):δ 1.00-1.18 (m,4H),3.52 (s,3H),.4.05-4.09 (m,1H),4.55-4.73 (m,4H),6.90 it,1H),7.89 (d,1H),8.75 (s,1H); 13C NMR (400 MHz,DMSO-d6):δ 9.3,36.4,40.8,48.8,50.6,105.6,107.3,108.9,114.7,117.3,118.6,119.9,131.0,135.3,137.7,144.0,147.4,151.3,165.3,175.7; HRMS-ESI m/z:450.13566 (calcd.for C20H19F3N5O4,450.13891[M+H] +).7g 1H NMR (400 MHz,CDCl3):δ 1.02-1.25 (m,4H),3.66 (s,3H),3.72 (s,3H),4.03-4.07 (m,i H),4.63-4.79 (m,4H),7.88 (d,1H),8.81 (s,1H);f3C NMR (400 MHz,DMSO-d6):δ 8.9,40.9,48.5,50.1,61.4,106.0,106.1,106.4,119.0,134.2,136.0,136.1,143.7,144.5,147.4,150.3,153.1,155.6,165.6,176.0; HRMS-ESI m/z:414.16054 (calcd.for C20H21FN5O4,4.

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药学进展
2012年 第10期

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