SYNTHESIS AND SAR OF PHENYLAZOLES, ACTIVE AGAINST <i>STAPHYLOCOCCUS AUREUS</i> NEWMAN

Authors

  • Vitalii V. Solomin Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia Riga Technical University, Faculty of Materials Science and Applied Chemistry, 3/7 Paula Valdena St., Riga LV-1048, Latvia
  • Blanca Fernandez Ciruelos Wageningen University & Research, Department of Animal Sciences, Droevendaalsesteeg 4, 6708 PB Wageningen, The Netherlands
  • Nadya Velikova Wageningen University & Research, Department of Animal Sciences, Droevendaalsesteeg 4, 6708 PB Wageningen, The Netherlands
  • Jerry Wells Wageningen University & Research, Department of Animal Sciences, Droevendaalsesteeg 4, 6708 PB Wageningen, The Netherlands
  • Marco Albanese Oxford Drug Design, Oxford Centre for Innovation, New Road, Oxford OX1 1BY, United Kingdom
  • Anmol Adhav Instituto de Biomedicina de Valencia CSIC, 11 Jaime Roig, Valencia 46010, Spain
  • Aigars Jirgensons Latvian Institute of Organic Synthesis, 21 Aizkraukles St., Riga LV-1006, Latvia Riga Technical University, Faculty of Materials Science and Applied Chemistry, 3/7 Paula Valdena St., Riga LV-1048, Latvia

DOI:

https://doi.org/10.1007/6885

Keywords:

diphenylazole, isoflavone, isoxazole, pyrazole, antimicrobial activity, Staphylococcus aureus Newman.

Abstract

Series of new potent inhibitors of growth of Staphylococcus aureus Newman, based on 3,4-diphenylpyrazole and 4,5-diphenylisoxazole derivatives were discovered. Structures of interest were selectively modified to check their structure–activity relationship. Studies revealed the most essential groups in the molecule for the antimicrobial activity retention. Active compounds with good MIC range should contain both nonpolar aromatic residues and hydrogen bond donating groups. The best MIC results in selected cases were lower than 1 μg/ml.

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Published

2022-12-20

Issue

Vol. 58 No. 12 (2022)

Section

Original Papers