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Molecules 2013, 18(7), 7557-7569; doi:10.3390/molecules18077557
Article

New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation

1
,
2
,
1
 and
1,*
1 School of Pharmacy, National Defense Medical Center, 161 Min-Chuan East Road, Section 6, Taipei 114, Taiwan 2 Department of Microbiology and Immunology, National Defense Medical Center, 161 Min-Chuan East Road, Section 6, Taipei 114, Taiwan
* Author to whom correspondence should be addressed.
Received: 5 June 2013 / Revised: 26 June 2013 / Accepted: 26 June 2013 / Published: 27 June 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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).
Keywords: antimicrobial agents; ciprofloxacin; ciprofloxacin-resistant Pseudomonas aeruginosa; methicillin-resistant Staphylococcus aureus antimicrobial agents; ciprofloxacin; ciprofloxacin-resistant Pseudomonas aeruginosa; methicillin-resistant Staphylococcus aureus
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Chen, P.-T.; Lin, W.-P.; Lee, A.-R.; Hu, M.-K. New 7-[4-(4-(un)Substituted)piperazine-1-carbonyl]- piperazin-1-yl] Derivatives of Fluoroquinolone: Synthesis and Antimicrobial Evaluation. Molecules 2013, 18, 7557-7569.

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