SAR study of 4-arylazo-3,5-diamino-1H-pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms
Reference: RSC Med Chem (2021) 12: 1868-1878

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 optimised, 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).

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Jansen C. U., Uhd J., Andersen J. B., Hultqvist L. D., Jakobsen T. H., Nilsson M., Nielsen T.E., Givskov M., Tolker-Nielsen T., Qvortrup K. M.