Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

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

Research output: Contribution to journalArticlepeer-review

Abstract

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

Original languageEnglish (US)
Pages (from-to)71-84
Number of pages14
JournalMedicinal chemistry (Shariqah (United Arab Emirates))
Volume17
Issue number1
DOIs
StatePublished - 2021

Keywords

  • amino acid
  • Antibacterial agents
  • antimicrobial
  • conjugates
  • fluoroquinolone
  • molecular modeling

ASJC Scopus subject areas

  • Drug Discovery

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