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

文献情報

出版日 2021-09-03

DOI 10.1039/D1MD00275A

インパクトファクター 0

著者

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

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要旨

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).

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RSC Medicinal Chemistry

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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

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RSC Medicinal Chemistry

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