Submit Manuscript  

Article Details


Synthesis of new Enrofloxacin Derivatives as Potential Antibiofilm Drugs Against Staphylococcus Aureus and Klebsiella Pneumoniae

Author(s):

Hina Siddiqui *, Haroon Mohamed Haniffa, Ayaz Ahmed and Muhammad Iqbal Choudhary*   Pages 1 - 12 ( 12 )

Abstract:


Background: The antimicrobial resistance due to biofilm formation among bacteria is a significant problem in the healthcare and food industries.

Objective: The current study describes the synthesis of enrofloxacin derivatives (2-17) and evaluation of their anti-bacterial and anti-biofilm activities.

Methods: Compounds 2-17 were synthesized through the acylation of enrofloxacin with thionyl chloride followed by reaction with different aromatic amines. The new analogues identified among the sixteen compounds were 2-7, 11, 14, and 17.

Results: Compound 2 appeared to be effective against pathogens S. aureus as well as K. pneumonia, whereas, compound 11 was found active against K. pneumonia only. Compound 2 inhibited >75% biofilm formation of S. aureus at 20 μg/mL and K. pneumonia at 10 μg/mL concentrations. These doses are far below the bactericidal concentration of compound 2 suggesting the anti-virulence mechanism of these compounds. Compound 11 inhibited 60% biofilm formation of K. pneumoniae at 70 μg/mL concentration. Compound 5 inhibited the biofilm of K. pneumoniae at 62 μg/mL concentration but also have bactericidal properties at this concentration. Interestingly, compounds 2 eradicated the preformed biofilm of both the pathogens at much lower doses as compared to control drug, gentamycin and substrate, enrofloxacin. Cytotoxicity of compounds 2– 17 was checked by standard method using 3T3 normal cell lines (mouse fibroblast), all compounds were found to be non-cytotoxic.

Conclusion: These compounds can be used alone or with FDA approved drugs to overcome biofilm related K. pneumoniae and S. aureus infections.

Keywords:

Enrofloxacin amide derivatives, Anti-biofilm, Antibacterial activity, Staphylococcus aureus, Klebsiella pneumoniae

Affiliation:

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270



Read Full-Text article