N-Pyridyl-Substituted Carboxypiperidine Amides: A New Class of Prokaryote Translation Inhibitors
| Autor: | Alina A. Sofronova, G. I. Filkov, V. A. Terent’ev, Ekaterina S. Komarova, Renat S. Yamidanov, A. G. Mazhuga, Ya. A. Ivanenkov, Olga A. Dontsova, Petr V. Sergiev, E. V. Deineka, Ilya A. Osterman |
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| Rok vydání: | 2019 |
| Předmět: |
Pharmacology
Reporter gene biology 010405 organic chemistry Chemistry Stereochemistry Translation (biology) Prokaryote biology.organism_classification 01 natural sciences Ribosome 0104 chemical sciences 010404 medicinal & biomolecular chemistry Drug Discovery Protein translation Antibacterial activity Selectivity Bacteria |
| Zdroj: | Pharmaceutical Chemistry Journal. 53:225-229 |
| ISSN: | 1573-9031 0091-150X |
| DOI: | 10.1007/s11094-019-01984-3 |
| Popis: | High-throughput screening identified a new class of antibacterial compounds based on N-pyridyl-substituted p- and m-carboxypiperidine amides. Constructs with the two reporter genes RFP and Katushka2S allowed the detection of compounds that inhibit protein translation against DNA biosynthesis. Some agents of this class demonstrated antibacterial activity by inhibiting translation. The most promising compound had an MIC of 12 μg/mL. Thus, this class could become a valuable platform for developing new compounds with higher antibacterial activity and selectivity. |
| Databáze: | OpenAIRE |
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