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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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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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