SAR study of 4-arylazo-3,5-diamino-1: H -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

doi:10.1039/d1md00275a

SAR study of 4-arylazo-3,5-diamino-1: H -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

Bacteriology

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

6 Citationer (Scopus)

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). This journal is

Originalsprog	Engelsk
Tidsskrift	RSC Medicinal Chemistry
Vol/bind	12
Udgave nummer	11
Sider (fra-til)	1868-1878
Antal sider	11
ISSN	2040-2503
DOI	https://doi.org/10.1039/d1md00275a
Status	Udgivet - 2021

Bibliografisk note

Publisher Copyright:
© The Royal Society of Chemistry.

Adgang til dokumentet

10.1039/d1md00275a

Citationsformater

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. (2021). SAR study of 4-arylazo-3,5-diamino-1: H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms. RSC Medicinal Chemistry, 12(11), 1868-1878. https://doi.org/10.1039/d1md00275a

SAR study of 4-arylazo-3,5-diamino-1 : H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms. / Jansen, Charlotte U.; Uhd, Jesper; Andersen, Jens B.; Hultqvist, Louise D.; Jakobsen, Tim H.; Nilsson, Martin ; Nielsen, Thomas E.; Givskov, Michael ; Tolker-Nielsen, Tim; Qvortrup, Katrine M.

I: RSC Medicinal Chemistry, Bind 12, Nr. 11, 2021, s. 1868-1878.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › peer review

Jansen, CU, Uhd, J, Andersen, JB , Hultqvist, LD , Jakobsen, TH , Nilsson, M , Nielsen, TE , Givskov, M , Tolker-Nielsen, T & Qvortrup, KM 2021, 'SAR study of 4-arylazo-3,5-diamino-1: H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms', RSC Medicinal Chemistry, bind 12, nr. 11, s. 1868-1878. https://doi.org/10.1039/d1md00275a

Jansen, Charlotte U. ; Uhd, Jesper ; Andersen, Jens B. ; Hultqvist, Louise D. ; Jakobsen, Tim H. ; Nilsson, Martin ; Nielsen, Thomas E. ; Givskov, Michael ; Tolker-Nielsen, Tim ; Qvortrup, Katrine M. / SAR study of 4-arylazo-3,5-diamino-1 : H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms. I: RSC Medicinal Chemistry. 2021 ; Bind 12, Nr. 11. s. 1868-1878.

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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). This journal is ",

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AU - Andersen, Jens B.

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AU - Jakobsen, Tim H.

AU - Nilsson, Martin

AU - Nielsen, Thomas E.

AU - Givskov, Michael

AU - Tolker-Nielsen, Tim

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