New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation
Fluoroquinolones have been a class of important synthetic antimicrobial agents broadly and effectively used in clinic for infectious diseases. In this study, the synthesis of a range of fluoroquinolone derivatives with 4-(carbopiperazin-1-yl)piperazinyl moieties at the C7 position and their inhibiti...
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2013-06-01
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Online Access: | http://www.mdpi.com/1420-3049/18/7/7557 |
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doaj-ca074cdcd0014a7b95371f73288983dc2020-11-24T22:27:20ZengMDPI AGMolecules1420-30492013-06-011877557756910.3390/molecules18077557New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial EvaluationMing-Kuan HuAn-Rong LeeWen-Po LinPo-Ting ChenFluoroquinolones have been a class of important synthetic antimicrobial agents broadly and effectively used in clinic for infectious diseases. In this study, the synthesis of a range of fluoroquinolone derivatives with 4-(carbopiperazin-1-yl)piperazinyl moieties at the C7 position and their inhibition of bacterial pathogens commonly disseminated in hospital environment were described. The results indicated that a 7-[4-(4-(benzoyl)carbopiperazin-1-yl)]piperazinyl derivative 5h and two 7-[4-(4- (benzenesulfonyl)carbopiperazin-1-yl)]piperazinyl derivatives 5k and 5l showed more promising growth inhibition of ciprofloxacin-resistant P. aeruginosa (CRPA) with MIC values as low as 16 mg/mL which is 16-fold more potent than ciprofloxacin, while most of other derivatives maintained potency against methicillin-resistant Staphylococcus aureus (MRSA).http://www.mdpi.com/1420-3049/18/7/7557antimicrobial agentsciprofloxacinciprofloxacin-resistant Pseudomonas aeruginosamethicillin-resistant Staphylococcus aureus |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Ming-Kuan Hu An-Rong Lee Wen-Po Lin Po-Ting Chen |
spellingShingle |
Ming-Kuan Hu An-Rong Lee Wen-Po Lin Po-Ting Chen New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation Molecules antimicrobial agents ciprofloxacin ciprofloxacin-resistant Pseudomonas aeruginosa methicillin-resistant Staphylococcus aureus |
author_facet |
Ming-Kuan Hu An-Rong Lee Wen-Po Lin Po-Ting Chen |
author_sort |
Ming-Kuan Hu |
title |
New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation |
title_short |
New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation |
title_full |
New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation |
title_fullStr |
New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation |
title_full_unstemmed |
New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation |
title_sort |
new 7-[4-(4-(un)substituted)piperazine-1-carbonyl]- piperazin-1-yl] derivatives of fluoroquinolone: synthesis and antimicrobial evaluation |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2013-06-01 |
description |
Fluoroquinolones have been a class of important synthetic antimicrobial agents broadly and effectively used in clinic for infectious diseases. In this study, the synthesis of a range of fluoroquinolone derivatives with 4-(carbopiperazin-1-yl)piperazinyl moieties at the C7 position and their inhibition of bacterial pathogens commonly disseminated in hospital environment were described. The results indicated that a 7-[4-(4-(benzoyl)carbopiperazin-1-yl)]piperazinyl derivative 5h and two 7-[4-(4- (benzenesulfonyl)carbopiperazin-1-yl)]piperazinyl derivatives 5k and 5l showed more promising growth inhibition of ciprofloxacin-resistant P. aeruginosa (CRPA) with MIC values as low as 16 mg/mL which is 16-fold more potent than ciprofloxacin, while most of other derivatives maintained potency against methicillin-resistant Staphylococcus aureus (MRSA). |
topic |
antimicrobial agents ciprofloxacin ciprofloxacin-resistant Pseudomonas aeruginosa methicillin-resistant Staphylococcus aureus |
url |
http://www.mdpi.com/1420-3049/18/7/7557 |
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