2. Academic Validation
  3. Synthesis and biological evaluation of 3,5-substituted pyrazoles as possible antibacterial agents

Synthesis and biological evaluation of 3,5-substituted pyrazoles as possible antibacterial agents

  • Bioorg Med Chem. 2021 Oct 15;48:116401. doi: 10.1016/j.bmc.2021.116401.
Matthew Payne 1,  Amy L Bottomley 2,  Anthony Och 1,  Anjar P Asmara 1,  Elizabeth J Harry 2,  Alison T Ung 3
Affiliations

Affiliations

  • 1 School of Mathematical and Physical Sciences, Faculty of Science, University of Technology Sydney, Broadway, NSW 2007, Australia.
  • 2 The ithree Institute, University of Technology Sydney, Broadway, NSW 2007, Australia.
  • 3 School of Mathematical and Physical Sciences, Faculty of Science, University of Technology Sydney, Broadway, NSW 2007, Australia. Electronic address: [email protected].
PMID: 34555556 DOI: 10.1016/j.bmc.2021.116401
Abstract

The emergence of multi-drug resistant bacteria has increased the need for novel Antibiotics to help overcome what may be considered the greatest threat to modern medicine. Here we report the synthesis of fifteen novel 3,5-diaryl-1H- pyrazoles obtained via one-pot cyclic oxidation of a chalcone and hydrazine-monohydrate. The synthesised pyrazoles were then screened against Staphylococcus aureus and Escherichia coli to determine their Antibacterial potential. The results show that compound 7p is bacteriostatic at MIC 8 µg/mL. The compound is non-toxic against healthy mammalian cells, 3T3-L1 at the highest test concentration 50 µg/mL. Furthermore, compound 7p significantly affected Bacterial morphogenesis before Cell Lysis in Bacillus subtilis when treated above the MIC concentration. From the results, a promising lead compound was identified for future development.

Keywords

Antibacterial; Bacterial morphology; Pyrazole; SAR.

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