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New 7-[4-(4-(un)substituted)piperazine-1-carbonyl]- piperazin-1-yl] derivatives of fluoroquinolone: synthesis and antimicrobial evaluation.

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

SUBMITTER: Chen PT

PROVIDER: S-EPMC6269787 | biostudies-literature | 2013 Jun

REPOSITORIES: biostudies-literature

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New 7-[4-(4-(un)substituted)piperazine-1-carbonyl]- piperazin-1-yl] derivatives of fluoroquinolone: synthesis and antimicrobial evaluation.

Chen Po-Ting PT Lin Wen-Po WP Lee An-Rong AR Hu Ming-Kuan MK

Molecules (Basel, Switzerland) 20130627 7

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- (b ...[more]

PMID: 23807580

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