Recent updates of fluoroquinolones as antibacterial agents. Issue 9 (26th July 2018)

• Record Type: Journal Article
• Authors: Ezelarab, Hend A. A.; Abbas, Samar H.; Hassan, Heba A.; Abuo‐Rahma, Gamal El‐Din A.
• Is Part Of: Archiv der Pharmazie. Volume 351:Issue 9(2018)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2018-07-26
• Subjects: antibacterial -- fluoroquinolones -- review -- structure–activity relationship; Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201800141
• Languages: English
• ISSNs: 0365-6233

Abstract

Abstract: Fluoroquinolones remain one of the most important kind of antibacterial agents used nowadays. The emergence of more virulent and resistant strains of bacteria by the development of either mutated DNA‐binding proteins or efflux pump mechanism for drugs is considered the main problem associated with the therapeutic use of these drugs. This situation participated in pushing researchers to design new fluoroquinolone derivatives, mainly with different substituents at C‐7 to withstand these resistant strains of bacteria and to obtain a wider spectrum of activity including activity against anaerobic organisms. Conjugation of fluoroquinolones with substitutions such as 1, 2, 4‐triazoles, alkyl oximes, flavonoids, aryl furans, benzofuroxans, metronidazoles or even other antibiotics such as neomycin‐B produced derivatives that have a superior and wider spectrum of activity and better resistance than the classical fluoroquinolone agents. Addition of a hydroxamic acid moiety to fluoroquinolones also increased the activity against Proteus mirabilis, which represents one of the most resistant strains of bacteria in urinary tract infections. This review aims to highlight the recent updates made for fluoroquinolones for broadening the spectrum of activity to become active not only against resistant strains of bacteria but also against anaerobic pathogens. Abstract : New fluoroquinolone derivatives are developed, mainly with different substituents at C‐7, to withstand resistant strains of bacteria and to obtain a wider spectrum of activity. Addition of a hydroxamic acid moiety increased the activity against Proteus mirabilis, one of the most resistant bacterial strains in urinary tract infections. This review highlights recent updates in the development of more active fluoroquinolones.