SAR study of 4-arylazo-3,5-diamino-1: H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms
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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.
In: RSC Medicinal Chemistry, Vol. 12, No. 11, 2021, p. 1868-1878.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - SAR study of 4-arylazo-3,5-diamino-1
T2 - H -pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms
AU - Jansen, Charlotte U.
AU - Uhd, Jesper
AU - Andersen, Jens B.
AU - Hultqvist, Louise D.
AU - Jakobsen, Tim H.
AU - Nilsson, Martin
AU - Nielsen, Thomas E.
AU - Givskov, Michael
AU - Tolker-Nielsen, Tim
AU - Qvortrup, Katrine M.
N1 - Publisher Copyright: © The Royal Society of Chemistry.
PY - 2021
Y1 - 2021
N2 - 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
AB - 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
U2 - 10.1039/d1md00275a
DO - 10.1039/d1md00275a
M3 - Journal article
C2 - 34841247
AN - SCOPUS:85119990587
VL - 12
SP - 1868
EP - 1878
JO - RSC Medicinal Chemistry
JF - RSC Medicinal Chemistry
SN - 2040-2503
IS - 11
ER -
ID: 286631232