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Synthesis and antimicrobial studies of azomethine and N-arylamine derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-methicillin-resistant Staphylococcus aureus agents

Abstract

Antimicrobial resistance to antibiotics is a global concern. Without urgent and coordinated action, the world is moving towards a post-antibiotic era, in which normal infections or minor injuries may become fatal. In an effort to find new agents to combat this resistance, we report the synthesis and antimicrobial activities of 1,3-diphenyl pyrazole derivatives. Several compounds have shown growth inhibition up to 24 mm in size against Staphylococcus aureus inhibition studies. We tested the active compounds against methicillin-resistant Staphylococcus aureus in minimum inhibitory concentration tests and found activity as low as 16 μg/mL.

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Acknowledgements

This work was supported by College of Science and Mathematics Arkansas State University, Jonesboro. Arkansas Statewide MS facility, Grant Number P30 GM103450 from the National Institute of General Medical Sciences of the National Institutes of Health (NIH) for recording mass spectra. This publication was made possible by the Arkansas INBRE program, supported by grant funding from the National Institutes of Health (NIH) National Institute of General Medical Sciences (NIGMS; P20 GM103429; formerly P20RR016460). Arkansas Biosciences Institute—Arkansas State University (ABI-A-state) start-up fund helped to complete this project. Anti-MRSA screening was performed by CO-ADD (The Community for Antimicrobial Drug Discovery), funded by the Welcome Trust (UK) and the University of Queensland (Australia).

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Correspondence to Mohammad A. Alam.

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Brider, J., Rowe, T., Gibler, D.J. et al. Synthesis and antimicrobial studies of azomethine and N-arylamine derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-methicillin-resistant Staphylococcus aureus agents. Med Chem Res 25, 2691–2697 (2016). https://doi.org/10.1007/s00044-016-1678-8

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Keywords

  • Pyrazole
  • Antimicrobials
  • Resistant
  • Imines
  • N-aryl amines
  • Antibacterial
  • Staphylococcus
  • Methicillin-resistant