N-Pyridyl-Substituted Carboxypiperidine Amides: A New Class of Prokaryote Translation Inhibitors
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.
Keywordsbacteria antibiotic ribosome screening reporter
The work was financially supported by the Ministry of Education and Science of the Russian Federation, Government Grant 20.9907.2017/VU (expert opinion, discussion, article preparation, selection of screening compounds), and the Russian Science Foundation, No. 17-74-30012, IBG, USC, RAS (HTS).
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