Abstract

SYNTHESIS, CHARACTERIZATION AND COMPUTATIONAL STUDIES OF GLYCINE SUBSTITUTED QUINOLONE ANALOGUES WITH POTENTIAL ANTIMICROBIAL AND ANTIOXIDANT ACTIVITY.

Anjoo Kamboj*, Harpreet Kaur and Upendra K. Jain

Abstract

Quinolones are a family of synthetic broad spectrum antimicrobial agents used worldwide; the main ophthalmic agents are ciprofloxacin and ofloxacin. Literature indicates that manipulation of the basic molecule, including replacing hydrogen with fluorine at position 6 and substituting new residues at position 1 of the quinolone ring, have led to improved antibacterial activity and pharmacokinetics. Different quinolone derivatives were synthesized by replacing carboglycine in place of 3-carboxylic acid group. The synthesized compounds were confirmed and characterized by physical, chemical tests, IR and 1HNMR spectral data. The test compounds were screened for their antibacterial and antifungal activity against Staphylococcus aureus, Streptococcus thermophilus (gram +ve bacterial strains), Escherichia coli, Pseudomonas aeruginosa (gram -ve bacterial strains), Candida albicans (fungal strain), Kluyveromyces marxianus (yeast) by cup plate method. The compound CG2 and CG5 showed good antibacterial activity and CG2 showed good antifungal activity. The antioxidant activity of synthesized test compounds was determine using DPPH method and H2O2 scavenging method. All the test compounds showed good antioxidant activity by DPPH method, in which CG4 was most active and CG2 least active. While by H2O2 method, CG5 was most active. Further from the assessment of structural similarity of target compounds with standard drugs and from QSAR studies performed using chem 3D ultra (version8.0.3, Cambridge software). It was concluded that all synthesized compounds showed good structural similarity with ciprofloxacin and norfloxacin.

Keywords: Quinolones, fluoroquinolones, antimicrobial activity, antioxidant activity, computational studies.