SAR study of 4-arylazo-3,5-diamino-1H-pyrazoles: identification of small molecules that induce dispersal of Pseudomonas aeruginosa biofilms
| Autor: | Louise Dahl Hultqvist, Martin Nilsson, Thomas E. Nielsen, Tim Tolker-Nielsen, Tim Holm Jakobsen, Charlotte Uldahl Jansen, Jens Bo Andersen, Michael Givskov, Jesper Uhd, Katrine Qvortrup |
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| Rok vydání: | 2021 |
| Předmět: |
Pharmacology
Pseudomonas aeruginosa Stereochemistry Aryl Organic Chemistry Biofilm Pharmaceutical Science Ring (chemistry) medicine.disease_cause Biochemistry Small molecule chemistry.chemical_compound chemistry Drug Discovery medicine Molecular Medicine heterocyclic compounds Pharmacophore Anti biofilm |
| Zdroj: | RSC Medicinal Chemistry. 12:1868-1878 |
| ISSN: | 2632-8682 |
| Popis: | 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). |
| Databáze: | OpenAIRE |
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