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

Charlotte U. Jansen, Jesper Uhd, Jens B. Andersen, Louise D. Hultqvist, Tim H. Jakobsen, Martin Nilsson, Thomas E. Nielsen, Michael Givskov, Tim Tolker-Nielsen, Katrine M. Qvortrup*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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).
Original languageEnglish
JournalRsc Medicinal Chemistry
Number of pages11
ISSN2632-8682
DOIs
Publication statusAccepted/In press - 2021

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