Fluoroquinolones: Blessings Or Curses

Abstract

: Fluoroquinolones are one of the world’s most valuable and popularly used categories of antimicrobial agents. This paper attempts to review the substantial progress of fluoroquinolones from its discovery to black box warning. Antibiotic drug choice will remain difficult in the presence of increasing resistance, but introduction of the fluoroquinolones has created a new and exciting era in antimicrobial treatment. These are a synthetic heterogeneous group of compounds used in both hospital and community practices to treat numerous severe infections. The era of quinolone antibiotics began with the serendipitous discovery of the quinolone prototype in 1962. The chronological development of fluoroquinolone reported that nalidixic acid was the first quinolone that gained popular choice for the treatment of urinary tract infection. The subsequent agents like levofloxacin, ofloxacin, norfloxacin, gatifloxacin, moxifloxacin, clinafloxacin, sparfloxacin, ciprofloxacin were derived through side chain and nuclear manipulation from basic pharmacphore. The fluoroquinolone motifs have been found as a milestone, is effective in certain infections are respiratory tract infection, urinary tract infection, bone disorders, meningococcal & mycobacterial infections, sexually transmitted diseases and skin infections etc. Fluoroquinolones are first entirely man made antibiotics exhibit antibacterial activity through the inhibition of topoisomerase II, topoisomerase IV and deoxy ribonucleic acid gyrase, which is vital for chromosome replication and function. The post marketing surveillance pointed out the favorable side effects associated with fluoroquinolones such as phototoxicity, QT interval prolongation and anaphylaxis. The discovery, development and clinical use of fluoroquinolone antibiotics in the last century contributed to a decline in morbidity and mortality rates.

Targeting SARS-CoV-2 RNA-dependent RNA polymerase: An in silico drug repurposing for COVID-19

“…Norfloxacin is a broad-spectrum fluoroquinolone antibiotic. Norfloxacin acts by blocking DNA gyrase and used to treat UTI 36 . Similar to quinolones, fluoroquinolones also found to modulate the cytokines, and this property is an added advantage in repurposing norfloxacin for COVID-19.…”

The perspective of antibiotic therapeutic challenges of brucellosis in the Middle East and North African countries: Current situation and therapeutic management

“…Fluoroquinolones are a group of broad‐spectrum bactericidal antibiotics that interfere with bacterial DNA synthesis (Majalekar & Shirote, 2020). Their in‐vitro activity against B. melitensis has been reported.…”

The replicative CMG helicase: the ideal target for cancer therapy

“…A separate study revealed that Ciprofloxacin directly intercalates with DNA [69], implicating that its inhibition may be due to a disturbance of the DNA structure, but not a direct effect on the helicase. Consistent with this mechanism, other DNA-associated enzymes, specifically topoisomerases, are known to be inhibited by fluoroquinolones [70]. Because during DNA replication topoisomerases progress in front of helicases and replicative machinery, it is topoisomerase activity that must be the most affected by the present of Ciprofloxacin.…”