Literature DB >> 31483233

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

Riham M Bokhtia1, Siva S Panda1, Adel S Girgis2, Hitesh H Honkanadavar1, Tarek S Ibrahim3, Riham F George4, Mona T Kashef5, Walid Fayad6, Rajeev Sakhuja7, Eatedal H Abdel-Aal3, Amany M M Al-Mahmoudy3.   

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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Entities:  

Keywords:  Antibacterial agents; amino acid; antimicrobial; conjugates; fluoroquinolone; molecular modeling

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Substances:

Year:  2021        PMID: 31483233     DOI: 10.2174/1573406415666190904143852

Source DB:  PubMed          Journal:  Med Chem        ISSN: 1573-4064            Impact factor:   2.745


  2 in total

1.  Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates.

Authors:  Riham M Bokhtia; Adel S Girgis; Tarek S Ibrahim; Fatma Rasslan; Eman S Nossier; Reham F Barghash; Rajeev Sakhuja; Eatedal H Abdel-Aal; Siva S Panda; Amany M M Al-Mahmoudy
Journal:  Pharmaceuticals (Basel)       Date:  2022-02-03

2.  New Pyrazine Conjugates: Synthesis, Computational Studies, and Antiviral Properties against SARS-CoV-2.

Authors:  Israa A Seliem; Adel S Girgis; Yassmin Moatasim; Ahmed Kandeil; Ahmed Mostafa; Mohamed A Ali; Mohamed S Bekheit; Siva S Panda
Journal:  ChemMedChem       Date:  2021-09-06       Impact factor: 3.540

  2 in total

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