Novel Glycoconjugate of 8-Fluoro Norfloxacin Derivativesas Gentamycin Resistant Staphylococcus aureus Inhibitors: Synthesis and Molecular Modeling Studies

Abstract

Antibiotic resistance has been the subject of interest in clinical practice due to high prevalence of antibiotic-resistant pathogenic organisms. In view of the prevalence of lesser resistance in antibiotics belonging to aminoglycoside class of compounds viz. Food and Drug administration (FDA) approved Gentamycin for the treatment of Stapphylococcus infections, which also has instances of resistance in the clinical isolates of S.aureus., a series of novel glycoconjugates of 8-fluoro Norfloxacin analogues with high regio-selectivity by employing copper (I)-catalyzed 1, 3-dipolar cycloaddition of 1-O-propargyl monosaccharides has been synthesized and evaluated for the antibacterial activity against gentamycin resistance S.aureus. Among these compounds, the compound 10g showed better antibacterial activity (MIC = 3.12 μg/ml) than gentamycin (E.coli (12.5 μg/ml), S. aureus (6.25 μg/ml), and K. pneumonia (6.25 μg/ml), including gentamycin resistant (>50 μg/ml) strain in vitro). The docking studies suggest DNA gyrase of S.aureus. as a probable target for the antibacterial action of compound 10g.