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

Autor:	Jansen CU; Department of Chemistry, Technical University of Denmark DK-2800 Lyngby Denmark kaqvo@kemi.dtu.dk., Uhd J; Department of Chemistry, Technical University of Denmark DK-2800 Lyngby Denmark kaqvo@kemi.dtu.dk., Andersen JB; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Hultqvist LD; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Jakobsen TH; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Nilsson M; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Nielsen TE; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark.; Singapore Centre for Environmental Life Sciences Engineering, Nanyang Technological University Singapore., Givskov M; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Tolker-Nielsen T; Costerton Biofilm Center, Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen DK-2200 Copenhagen Denmark., Qvortrup KM; Department of Chemistry, Technical University of Denmark DK-2800 Lyngby Denmark kaqvo@kemi.dtu.dk.
Jazyk:	angličtina
Zdroj:	RSC medicinal chemistry [RSC Med Chem] 2021 Sep 03; Vol. 12 (11), pp. 1868-1878. Date of Electronic Publication: 2021 Sep 03 (Print Publication: 2021).
DOI:	10.1039/d1md00275a
Abstrakt:	By screening of a collection of 50 000 small-molecule compounds, we recently identified 4-arylazo-3,5-diamino-1 H -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-1 H -pyrazol-3-amine ( 2 ). Competing Interests: There is no conflict of interest to declare. (This journal is © The Royal Society of Chemistry.)
Databáze:	MEDLINE
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