Fluoroquinolones structural and medicinal developments (2013-2018): Where are we now?
Ghadeer A R Y Suaifan1, Aya A M Mohammed1
1Department of Pharmaceutical Sciences, Faculty of Pharmacy, The University of Jordan, Amman 11942, Jordan.
Bioorganic & Medicinal Chemistry
|June 12, 2019
Summary
Newer fluoroquinolones show promise, but rising bacterial resistance necessitates exploring novel derivatives. This study reviews structure-activity relationships for antibacterial, anticancer, and antifungal fluoroquinolone activities.
Area of Science:
- Medicinal Chemistry
- Pharmacology
- Drug Discovery
Background:
- Fluoroquinolones are crucial antibiotics, with newer generations offering enhanced efficacy.
- Increasing bacterial resistance worldwide drives the need for novel antimicrobial agents.
- Quinolone scaffolds exhibit diverse biological activities, including antimicrobial and anticancer properties.
Purpose of the Study:
- To review structure-activity relationships (SAR) of fluoroquinolone derivatives.
- To discuss antibacterial, anticancer, and antifungal activities of fluoroquinolones.
- To highlight research trends and arguments in fluoroquinolone SAR from 2013-2015.
Main Methods:
- Literature review of scientific publications (2013-2015).
- Analysis of structure-activity relationships for fluoroquinolone derivatives.
- Synthesis of guided-biologically-oriented strategies.
Main Results:
- Newer fluoroquinolones (moxifloxacin, delafloxacin, finafloxacin) demonstrate broader spectra and better bioavailability.
- Quinolone derivatives show potential as novel antimicrobial and anticancer agents.
- Opposing arguments regarding fluoroquinolone SAR were identified and discussed.
Conclusions:
- Fluoroquinolone SAR is a dynamic field with ongoing research into novel derivatives.
- Understanding SAR is critical for developing new agents to combat bacterial resistance.
- Fluoroquinolones hold promise beyond antibacterial applications, including anticancer and antifungal uses.
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