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Design, Synthesis, and Antibacterial Activities of Novel Heterocyclic Arylsulphonamide Derivatives

  • Anuradha Singh
  • Ritika Srivastava
  • Ramendra K. Singh
Original Research Article

Abstract

Design, synthesis, and antibacterial activities of a series of arylsulphonamide derivatives as probable peptide deformylase (PDF) inhibitors have been discussed. Compounds have been designed following Lipinski’s rule and after docking into the active site of PDF protein (PDB code: 1G2A) synthesized later on. Furthermore, to assess their antibacterial activity, screening of the compound was done in vitro conditions against Gram-positive and Gram-negative bacterial strains. In silico, studies revealed these compounds as potential antibacterial agents and this fact was also supported by their prominent scoring functions. Antibacterial results indicated that these molecules possessed a significant activity against Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, and Escherichia coli with MIC values ranging from 0.06 to 0.29 μM. TOPKAT results showed that high LD50 values and the compounds were assumed non-carcinogenic when various animal models were studied computationally.

Keywords

Arylsulphonamides Peptide deformylase inhibitors Antibacterial activity SAR QSTR 

Notes

Acknowledgements

Financial assistance in the form of WOS-A fellowship (SR/WOS-A/CS-1053/2014) to Anuradha Singh by the DST, New Delhi is sincerely acknowledged.

Compliance with ethical standards

Conflict of interest

The author(s) declare no competing interests.

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Copyright information

© International Association of Scientists in the Interdisciplinary Areas and Springer-Verlag Berlin Heidelberg 2017

Authors and Affiliations

  • Anuradha Singh
    • 1
  • Ritika Srivastava
    • 1
  • Ramendra K. Singh
    • 1
  1. 1.Bioorganic Research Laboratory, Department of ChemistryUniversity of AllahabadAllahabadIndia

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