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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.
A series of potent and less toxic, 5-{[((5-substituted aryl)-1,3,4-thiadiazol-2-yl) thio]-n-alkyl}-1,3,4-oxadiazole-2-thiol was synthesized. Each compound was evaluated for anti-inflammatory activity by carrageenan-induced rat paw oedema method. Compounds PS1, PS4, PS9, and PS12 showed comparatively potent anti-inflammatory activity as compared to control as well as other test compounds. These potent compounds were also tested for acute ulcerogenic activity. Results of both studies were found statistically significant.
The novel Pyrazoline derivatives were prepared by cyclisation of substituted chalcone derivatives in the presence of 2, 4 dintro phenyl hydrazine hydrate. Structural elucidation of all synthesized derivatives were done by spectral analysis ( IR , NMR and Mass spectroscopy). All synthesized derivatives screened for their anticancer activities by MTT assay and these prepared derivatives exhibits promising anticancer activities.
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