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

Molecules

Po-Ting Chen²  Wen-Po Lin¹  An-Rong Lee² 

[1] Department of Microbiology and Immunology, National Defense Medical Center, 161 Min-Chuan East Road, Section 6, Taipei 114, Taiwan; E-Mail:;School of Pharmacy, National Defense Medical Center, 161 Min-Chuan East Road, Section 6, Taipei 114, Taiwan; E-Mails:

关键词: antimicrobial agents;    ciprofloxacin;    ciprofloxacin-resistant Pseudomonas aeruginosa;    methicillin-resistant Staphylococcus aureus;   

DOI  :  10.3390/molecules18077557

来源: mdpi

【 摘 要 】

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 μg/mL which is 16-fold more potent than ciprofloxacin, while most of other derivatives maintained potency against methicillin-resistant Staphylococcus aureus (MRSA).

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.