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.
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