N-Pyridyl-Substituted Carboxypiperidine Amides: A New Class of Prokaryote Translation Inhibitors

Ya A. Ivanenkov, E. S. Komarova (Andreyanova), I. A. Osterman, P. V. Sergiev, R. S. Yamidanov, E. V. Deineka, V. A. Terent’ev, G. I. Fil’kov, A. A. Sofronova, A. G. Mazhuga, O. A. Dontsova

    Research output: Contribution to journalArticlepeer-review

    2 Citations (Scopus)

    Abstract

    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.

    Original languageEnglish
    Pages (from-to)225-229
    Number of pages5
    JournalPharmaceutical Chemistry Journal
    Volume53
    Issue number3
    DOIs
    Publication statusPublished - 15 Jun 2019

    Keywords

    • antibiotic
    • bacteria
    • reporter
    • ribosome
    • screening

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