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Fluoroquinolone-3-carboxamide amino acid conjugates: Synthesis, antibacterial properties and molecular modeling studies

Author(s):

Riham M. Bokhtia, Siva S. Panda*, Adel S. Girgis, Hitesh H. Honkanadavar, Tarek S. Ibrahim, Amany M. M. Al-Mahmoudy, Riham F. George, Mona T. Kashef, Walid Fayad, Rajeev Sakhuja and Eatedal H. Abdel-Aal  

Abstract:


Background: Bacterial infections are considered as one of the major global health threat, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents.

Method: The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates.

Result: All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433).

Conclusion: The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.

Keywords:

Fluoroquinolone, Amino acid, Conjugates, Antimicrobial, Molecular modeling

Affiliation:

Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre, Dokki, Giza, 12622, Department of Chemistry, Birla Institute of Technology and Science, Pilani 333 031, Rajasthan, Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig, 44519



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