Ciprofloxacin derivatives and their antibacterial activities

Bacterial infections represent a significant health threat globally, and are responsible for the majority of hospital-acquired infections, leading to extensive mortality and burden on global healthcare systems. The second generation fluoroquinolone ciprofloxacin which exhibits excellent antimicrobia...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2018-02, Vol.146, p.599-612
Main Authors: Zhang, Gui-Fu, Liu, Xiaofeng, Zhang, Shu, Pan, Baofeng, Liu, Ming-Liang
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial
Ciprofloxacin
Ciprofloxacin - chemical synthesis
Ciprofloxacin - chemistry
Ciprofloxacin - pharmacology
Dose-Response Relationship, Drug
Fluoroquinolones
Gram-Negative Bacteria - drug effects
Gram-Positive Bacteria - drug effects
Hybrid compounds
Molecular Structure
Structure-Activity Relationship
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Summary:Bacterial infections represent a significant health threat globally, and are responsible for the majority of hospital-acquired infections, leading to extensive mortality and burden on global healthcare systems. The second generation fluoroquinolone ciprofloxacin which exhibits excellent antimicrobial activity and pharmacokinetic properties as well as few side effects is introduced into clinical practice for the treatment of various bacterial infections for around 3 decades. The emergency and widely spread of drug-resistant pathogens making ciprofloxacin more and more ineffective, so it's imperative to develop novel antibacterials. Numerous of ciprofloxacin derivatives have been synthesized for seeking for new antibacterials, and some of them exhibited promising potency. This review aims to summarize the recent advances made towards the discovery of ciprofloxacin derivatives as antibacterial agents and the structure-activity relationship of these derivatives was also discussed. This review aims to outline the antibacterial activity of ciprofloxacin derivatives, and discuss their structure-activity relationship to pave the way for the further rational development. [Display omitted] •The recent advances in ciprofloxacin derivatives as antibacterial agents were summarized.•Some ciprofloxacin derivatives exhibited promising in vitro and in vivo antibacterial potency.•The structure-activity relationship was also discussed.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2018.01.078