| 1-乙基-6-氟-1,4-二氢-4-氧-7-(4-对硝基苯甲酰基-1-哌嗪基)喹啉-3-羧酸及其类似物的合成 |
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| 引用本文： | 陈恒昌,郭彦春,路德让.1-乙基-6-氟-1,4-二氢-4-氧-7-(4-对硝基苯甲酰基-1-哌嗪基)喹啉-3-羧酸及其类似物的合成[J].药学学报,1991(4). |
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| 作者姓名： | 陈恒昌 郭彦春 路德让 |
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| 作者单位： | 郑州大学化学系，郑州大学化学系，郑州大学化学系 郑州 450052，郑州 450052，郑州 450052 |
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| 摘 要： | 氟哌酸(norfloxacin)是吡酮酸类药物的优秀代表之一,其特点是抗菌谱广,抗菌作用强,该药对绿脓杆菌的作用较庆大霉素强,并远优于萘啶酸和吡哌酸,但美中不足的是易于代谢和体内生物利用度及血浓度较低,从而影响了实际效果。为了改善疗效,根据药物在体内作用和代谢以及口服给药的特点,设计合成了系列氟哌酸的新类似物,以期通过改造化合物结构来改变化合物的理化性质,体内代谢途径,获得血浓度和活性高、毒副作用小,疗效更好的抗菌药物。合成路线如下:
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SYNTHESES OF 1-ETHYL-6-FLUORO-1,4-DIHYDRO-4-OXO-7-[(4-P-NITROBENZOL)-1-PIPERAZINYL] QUINOLINE-3-CARBOXYLIC ACID AND ITS ANALOGUES |
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| HC Chen YC Guo and DR Lu.SYNTHESES OF 1-ETHYL-6-FLUORO-1,4-DIHYDRO-4-OXO-7-[(4-P-NITROBENZOL)-1-PIPERAZINYL] QUINOLINE-3-CARBOXYLIC ACID AND ITS ANALOGUES[J].Acta Pharmaceutica Sinica,1991(4). |
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| Authors: | HC Chen YC Guo and DR Lu |
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| Abstract: | Syntheses of thirteen new compounds of 1-ethyl-6-flouro-1, 4 - dihydro - 4 - oxo - 7 - (4- p- nitrobenzoyl)1 - piperazinyl] quinoline - 3 - carboxylic acid and its analogues are reported. The structures were determined by IR, ~1HNMR and elemental analysis, Four compounds have been subjected to antibacterial activity tests in vitro. Compound I_1 was shown to have significant activity. |
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| Keywords: | Antibacterial agents Pyridonecarboxylic acids Quinoline derivatives |
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