Novel fluorinated piperazine based-amino acid derivatives as antiplasmodial agents: Synthesis, bioactivity and computational studies

Authors

  • Charu Upadhyay University of Delhi
  • Shreya Bhattacharya National Institute of Immunology
  • Sumit Kumar University of Delhi
  • Dharmender Kumar University of Delhi
  • Neha Bhadula University of Delhi
  • Brijesh Rathi University of Delhi
  • Agam Prasad Singh National Institute of Immunology
  • Poonam Singh University of Delhi

Keywords:

Plasmodium falciparum, anti-malarial drugs, heteroaromatic amino acid, antimalarial agent, in-silico studies

Abstract

A library of twenty novel analogues of fluorinated, N-(3-hydroxy-1-phenyl-4-(4-phenylpiperazin-1-yl)alkyl)amides containing different amino acids were synthesized and tested for the activity against Plasmodium falciparum (Pf3D7) culture. All the tested compounds showed TC50 values >100 µM on HepG2 cells. Hit analogues 12c and 12e, displayed IC50 values in the sub-micromolar range, i.e., 0.696±0.0462 µM and 0.9377±0.0461 µM, respectively. Compounds 12c and 12e were also evaluated in combination with artemisinin, which slightly improved the activity of both the compounds with IC50 values of 0.19 µM and 0.26 µM, respectively. For compounds 12c and 12e, in-silico studies were carried out. Overall, results obtained from both in vitro and in-silico studies, indicated that 12c and 12e were hit compounds with maximum potency.

URN:NBN:sciencein.cbl.2023.v10.543

Author Biographies

  • Charu Upadhyay, University of Delhi

    Department of Chemistry
    Miranda House

  • Shreya Bhattacharya, National Institute of Immunology

    Infectious Diseases Laboratory

  • Sumit Kumar, University of Delhi

    Department of Chemistry,
    Miranda House

  • Dharmender Kumar, University of Delhi

    Department of Chemistry,
    Miranda House

  • Neha Bhadula, University of Delhi

    Department of Chemistry,
    Miranda House

  • Brijesh Rathi, University of Delhi

    Department of Chemistry
    Hansraj College
    https://vidwan.inflibnet.ac.in/profile/292386

  • Agam Prasad Singh, National Institute of Immunology

    Infectious Diseases Laboratory

  • Poonam Singh, University of Delhi

    Department of Chemistry
    Miranda House

    Delhi School of Public Health, Institute of Eminence, University of Delhi

fluorinated piperazine-amino acid as antimalarials

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Published

2023-03-20

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How to Cite

Novel fluorinated piperazine based-amino acid derivatives as antiplasmodial agents: Synthesis, bioactivity and computational studies. (2023). Chemical Biology Letters, 10(3), 543. https://pubs.thesciencein.org/journal/index.php/cbl/article/view/a543

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