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.