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SAR study of 4-arylazo-3,5-diamino-1H-pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms.

Charlotte Uldahl JansenJesper UhdJens B AndersenLouise D HultqvistTim Holm JakobsenMartin NilssonThomas E NielsenMichael GivskovTim Tolker-NielsenKatrine M Qvortrup
Published in: RSC medicinal chemistry (2021)
By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1H-pyrazoles as a novel group of anti-biofilm agents. Here, we report a SAR study based on 60 analogues by examining ways in which the pharmacophore can be further optimized, for example, via substitutions in the aryl ring. The SAR study revealed the very potent anti-biofilm compound 4-(2-(2-fluorophenyl)hydrazineylidene)-5-imino-4,5-dihydro-1H-pyrazol-3-amine (2).
Keyphrases
  • pseudomonas aeruginosa
  • small molecule
  • staphylococcus aureus
  • candida albicans
  • cystic fibrosis
  • molecular docking
  • multidrug resistant