Abstract
New synthetic 36 fluoroquinolones (FQs) have been developed. Their anti-inflammatory and 2,2-diphenyl-1-picrylhydrazyl (DPPH)- and nitric oxide (NO)- radicals scavenging propensities were delineated in vitro. The anti-inflammation related NO radical scavenging bioactivities of new FQs compounds against lipopolysaccharide (LPS)-prompted NO production in RAW 264.7 macrophages were examined using the Griess assay. Selectively nitro FQ compound 2-AnisCEtA exerted an exceedingly superior anti-inflammatory effects (p<0.001 vs. indomethacin IC50 value of 103.35±4.4 μM) while 7 nitro FQs, 10 reduced FQs and 9 triazolo FQs were moderately more efficacious than indomethacin. The remaining 9 Compounds could display appreciable anti-inflammatory capacity. Unequivocally their DPPH radical scavenging effects were of substantially lesser efficacy than ascorbic acid. Using 400 μM methylglyoxal as the choice glucotoxicity concentration in RAW264.7 macrophages; it was shown that 18 out of 36 FQs could exhibit an exceedingly more superior than or significantly comparable cytoprotection against methylglyoxal-induced carbonyl toxicity to antiglycation aminoguanidine. Suggestively dual modulation of glycation-inflammation can be linked with FQs lipophilicity-chelating properties. FQs can serve as scaffolds for the development and designing of new druggable deglycation and antiglycation therapeutic candidates via duality of antiglycation-antiinflammatory capacities.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
