Affiliation:
1. Department of Pharmaceutical Chemistry, Appasaheb Birnale College of Pharmacy, Sangli. Shivaji University, Sangli – 416416, India
2. Department of Pharmaceutical Chemistry, Arvind Gavali College of Pharmacy, Satara Shivaji University, Satara- 415015, India
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
their discovery to black box warning. Antibiotic drug choice will remain difficult in the presence of
increasing resistance, but the introduction of 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, and ciprofloxacin were derived
through side chain and nuclear manipulation from basic pharmacophore. The fluoroquinolone motifs
have been found as a milestone, effective in certain infections that are respiratory tract infection, urinary
tract infection, bone disorders, meningococcal and mycobacterial infections, sexually transmitted
diseases, skin infections, etc. Fluoroquinolones are first entirely man-made antibiotics that exhibit antibacterial
activity through the inhibition of topoisomerase II, topoisomerase IV and deoxyribonucleic
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.
Publisher
Bentham Science Publishers Ltd.
Subject
Clinical Biochemistry,Drug Discovery,Pharmacology,Molecular Medicine
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