Abstract

Development of novel derivatives to rein in and fight bacteria have never been more demanding, as microbial resistance strains are alarmingly increasing. A multitude of new fluoroquinolones derivatives with an improved spectrum of activity and/or enhanced pharmacokinetics parameters have been widely explored. Reporting novel antimicrobial agents entails comparing their potential activity to their parent drugs; hence, parent fluoroquinolones have been used in research as positive controls. Given that these fluoroquinolones possess variable activities according to their generation, it is necessary to include parent compounds and market available antibiotics of the same class when investigating antimicrobial activity. Herein, we provide a detailed guide on the in vitro biological activity of fluoroquinolones based on experimental results published in the last years. This work permits researchers to compare and analyze potential fluoroquinolones as positive control agents and to evaluate changes occurring in their activities. More importantly, the selection of fluoroquinolones as positive controls by medicinal chemists when investigating novel FQs analogs must be correlated to the laboratory pathogen inquest for reliable results.

Highlights

  • Academic Editor: Jean-MarcAntimicrobial prescriptions for the treatment of infections caused in particular by Staphylococcus aureus (S. aureus), Pseudomonas aeruginosa (P. aeruginosa), and Mycobacterium tuberculosis (M. tuberculosis) have been affected by bacterial resistance [1]

  • Antiviral, antifungal agents in addition to their antibacterial activity where the latter is attributed to their ability to selectively inhibit bacterial type II topoisomerases, Currently, FQs are one of thePharmocokinetic most widely properties used antimicrobial drugs, with a wide potency range of indications, covering respiratoryand infections, urinary tract infections (UTIs), gastrointestinal infections, and gynecologic infections

  • Can only approximate minimum inhibitory concentration (MIC) based on diameter of the zones of inhibition

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Summary

Introduction

Antimicrobial prescriptions for the treatment of infections caused in particular by Staphylococcus aureus (S. aureus), Pseudomonas aeruginosa (P. aeruginosa), and Mycobacterium tuberculosis (M. tuberculosis) have been affected by bacterial resistance [1]. Literature reviews pointed out FQs’ potential activities as anticancer, antitumor, antiviral, and antifungal agents in addition to their antibacterial activity where the latter is attributed to their ability to selectively inhibit bacterial type II topoisomerases, DNA gyrase, and/or topoisomerase IV [12–15]. FQs are one of the most widely used antimicrobial drugs, with a wide range of indications, covering respiratory infections, urinary tract infections (UTIs), gastrointestinal infections, and gynecologic infections [16]. Antiviral, antifungal agents in addition to their antibacterial activity where the latter is attributed to their ability to selectively inhibit bacterial type II topoisomerases, Currently, FQs are one of thePharmocokinetic most widely properties used antimicrobial drugs, with a wide potency range of indications, covering respiratoryand infections, urinary tract infections (UTIs), gastrointestinal infections, and gynecologic infections [16].

Fluoroquinolone’s
Spectrum
Comparison of the In Vitro Antimicrobial Assays
FQ’s Antibacterial Activity against Gram-Positive Bacteria
FQs Antibacterial Activity against Gram-Negative Bacteria
FQs’ Antimycobacterial Activity
FQs’ Antifungal, Antiparasitic, and Anticancer Activity
FQs Inhibitory Effect as Anti-Viral Agaents against SARS-CoV-2 and HIV-1
Recommendations
Methods

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