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Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation

The evolution of the class of antibacterial quinolones includes the introduction in therapy of highly successful compounds. Although many representatives were withdrawn due to severe adverse reactions, a few representatives have proven their therapeutical value over time. The classification of antib...

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Autores principales: Rusu, Aura, Lungu, Ioana-Andreea, Moldovan, Octavia-Laura, Tanase, Corneliu, Hancu, Gabriel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8399897/
https://www.ncbi.nlm.nih.gov/pubmed/34452252
http://dx.doi.org/10.3390/pharmaceutics13081289
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author Rusu, Aura
Lungu, Ioana-Andreea
Moldovan, Octavia-Laura
Tanase, Corneliu
Hancu, Gabriel
author_facet Rusu, Aura
Lungu, Ioana-Andreea
Moldovan, Octavia-Laura
Tanase, Corneliu
Hancu, Gabriel
author_sort Rusu, Aura
collection PubMed
description The evolution of the class of antibacterial quinolones includes the introduction in therapy of highly successful compounds. Although many representatives were withdrawn due to severe adverse reactions, a few representatives have proven their therapeutical value over time. The classification of antibacterial quinolones into generations is a valuable tool for physicians, pharmacists, and researchers. In addition, the transition from one generation to another has brought new representatives with improved properties. In the last two decades, several representatives of antibacterial quinolones received approval for therapy. This review sets out to chronologically outline the group of approved antibacterial quinolones since 2000. Special attention is given to eight representatives: besifloxacin, delafoxacin, finafloxacin, lascufloxacin, nadifloxacin and levonadifloxacin, nemonoxacin, and zabofloxacin. These compounds have been characterized regarding physicochemical properties, formulations, antibacterial activity spectrum and advantageous structural characteristics related to antibacterial efficiency. At present these new compounds (with the exception of nadifloxacin) are reported differently, most often in the fourth generation and less frequently in a new generation (the fifth). Although these new compounds’ mechanism does not contain essential new elements, the question of shaping a new generation (the fifth) arises, based on higher potency and broad spectrum of activity, including resistant bacterial strains. The functional groups that ensured the biological activity, good pharmacokinetic properties and a safety profile were highlighted. In addition, these new representatives have a low risk of determining bacterial resistance. Several positive aspects are added to the fourth fluoroquinolones generation, characteristics that can be the basis of the fifth generation. Antibacterial quinolones class continues to acquire new compounds with antibacterial potential, among other effects. Numerous derivatives, hybrids or conjugates are currently in various stages of research.
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spelling pubmed-83998972021-08-29 Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation Rusu, Aura Lungu, Ioana-Andreea Moldovan, Octavia-Laura Tanase, Corneliu Hancu, Gabriel Pharmaceutics Review The evolution of the class of antibacterial quinolones includes the introduction in therapy of highly successful compounds. Although many representatives were withdrawn due to severe adverse reactions, a few representatives have proven their therapeutical value over time. The classification of antibacterial quinolones into generations is a valuable tool for physicians, pharmacists, and researchers. In addition, the transition from one generation to another has brought new representatives with improved properties. In the last two decades, several representatives of antibacterial quinolones received approval for therapy. This review sets out to chronologically outline the group of approved antibacterial quinolones since 2000. Special attention is given to eight representatives: besifloxacin, delafoxacin, finafloxacin, lascufloxacin, nadifloxacin and levonadifloxacin, nemonoxacin, and zabofloxacin. These compounds have been characterized regarding physicochemical properties, formulations, antibacterial activity spectrum and advantageous structural characteristics related to antibacterial efficiency. At present these new compounds (with the exception of nadifloxacin) are reported differently, most often in the fourth generation and less frequently in a new generation (the fifth). Although these new compounds’ mechanism does not contain essential new elements, the question of shaping a new generation (the fifth) arises, based on higher potency and broad spectrum of activity, including resistant bacterial strains. The functional groups that ensured the biological activity, good pharmacokinetic properties and a safety profile were highlighted. In addition, these new representatives have a low risk of determining bacterial resistance. Several positive aspects are added to the fourth fluoroquinolones generation, characteristics that can be the basis of the fifth generation. Antibacterial quinolones class continues to acquire new compounds with antibacterial potential, among other effects. Numerous derivatives, hybrids or conjugates are currently in various stages of research. MDPI 2021-08-18 /pmc/articles/PMC8399897/ /pubmed/34452252 http://dx.doi.org/10.3390/pharmaceutics13081289 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Rusu, Aura
Lungu, Ioana-Andreea
Moldovan, Octavia-Laura
Tanase, Corneliu
Hancu, Gabriel
Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title_full Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title_fullStr Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title_full_unstemmed Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title_short Structural Characterization of the Millennial Antibacterial (Fluoro)Quinolones—Shaping the Fifth Generation
title_sort structural characterization of the millennial antibacterial (fluoro)quinolones—shaping the fifth generation
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8399897/
https://www.ncbi.nlm.nih.gov/pubmed/34452252
http://dx.doi.org/10.3390/pharmaceutics13081289
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