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Antistaphylococcal Triazole-Based Molecular Hybrids: Design, Synthesis and Activity.

Kostiantyn Shabelnyk1, Alina Fominichenko2, Oleksii Antypenko1

  • 1Department of Pharmaceutical, Organic and Bioorganic chemistry, Zaporizhzhia State Medical and Pharmaceutical University, 69000 Zaporizhzhia, Ukraine.

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Summary

New hybrid molecules, [2-(3-R-1H-[1,2,4]-triazol-5-yl)phenyl]amines, show potent antistaphylococcal activity. These compounds, targeting DNA gyrase, offer a promising avenue for developing novel antibacterial agents against resistant Staphylococcus aureus strains.

Keywords:
antistaphylococcal activitymolecular dockingtriazole«one-pot» synthesis

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Area of Science:

  • Medicinal Chemistry
  • Organic Synthesis
  • Antimicrobial Drug Discovery

Background:

  • The rise of antibiotic resistance necessitates the development of novel small molecules with targeted activity against specific bacterial pathogens.
  • A strategy was developed to synthesize novel hybrid molecules, specifically [2-(3-R-1H-[1,2,4]-triazol-5-yl)phenyl]amines, as potential antibacterial agents.
  • These compounds are designed as building blocks for introducing structural motifs to enhance antistaphylococcal effects.

Purpose of the Study:

  • To synthesize and evaluate the antistaphylococcal activity of novel [2-(3-R-1H-[1,2,4]-triazol-5-yl)phenyl]amine derivatives.
  • To investigate the potential molecular mechanism of action, including DNA gyrase inhibition.
  • To explore structure-activity relationships (SAR) and pharmacokinetic properties (ADME) to guide further development.

Main Methods:

  • One-pot synthesis of [2-(3-R-1H-[1,2,4]-triazol-5-yl)phenyl]amines from substituted 4-hydrazinoquinazolines or 2-aminobenzonitriles.
  • Molecular docking studies to predict the mechanism of action as DNA gyrase inhibitors.
  • Determination of minimum inhibitory concentrations (MIC) against Staphylococcus aureus.
  • Structure-activity relationship (SAR) and ADME analyses.

Main Results:

  • Several synthesized compounds exhibited significant antibacterial activity against Staphylococcus aureus, with MICs ranging from 10.1-62.4 µM.
  • Two compounds, 5-bromo-2-(3-(furan-3-yl)-1H-1,2,4-triazol-5-yl)aniline and 5-fluoro-2-(3-(thiophen-3-yl)-1H-1,2,4-triazol-5-yl)aniline, showed potent activity (MICs of 5.2 and 6.1 µM, respectively), comparable to Ciprofloxacin (MIC: 4.7 µM).
  • SAR analysis indicated that cycloalkyl or electron-rich heterocyclic fragments at the triazole ring's third position are crucial for activity. Methylation of the aniline moiety enhanced activity, while halogen introduction had variable effects.

Conclusions:

  • The synthesized [2-(3-R-1H-[1,2,4]-triazol-5-yl)phenyl]amines demonstrate significant antistaphylococcal activity.
  • These compounds represent promising candidates for further investigation as novel antibacterial agents.
  • Structural modifications, particularly incorporating specific fragments and substituents, can optimize antistaphylococcal efficacy.