Issue 11, 2021

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

Abstract

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).

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

Supplementary files

Article information

Article type
Research Article
Submitted
16 Aug 2021
Accepted
30 Aug 2021
First published
03 Sep 2021

RSC Med. Chem., 2021,12, 1868-1878

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

C. U. Jansen, J. Uhd, J. B. Andersen, L. D. Hultqvist, T. H. Jakobsen, M. Nilsson, T. E. Nielsen, M. Givskov, T. Tolker-Nielsen and K. M. Qvortrup, RSC Med. Chem., 2021, 12, 1868 DOI: 10.1039/D1MD00275A

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