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


Citar

Texto integral

Acesso aberto Acesso aberto
Acesso é fechado Acesso está concedido
Acesso é fechado Somente assinantes

Resumo

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.

Sobre autores

Ya. Ivanenkov

Moscow Institute of Physics and Technology (State University); Department of Chemistry, M. V. Lomonosov Moscow State University; Institute of Biochemistry and Genetics, Ufa Scientific Center, Russian Academy of Sciences

Email: ekaterina.deyneka@phystech.edu
Rússia, 9 Institutskii Pereul., Moscow Region, Dolgoprudnyi, 141700; 1/3 Leninskie Gory, Moscow, 119991; 71 Prosp. Oktyabrya, Ufa, Republic of Bashkortostan, 450054

E. Komarova (Andreyanova)

A. N. Belozersky Research Institute of Physico-Chemical Biology, M. V. Lomonosov Moscow State University

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/40, Leninskie Gory, Moscow, 119992

I. Osterman

A. N. Belozersky Research Institute of Physico-Chemical Biology, M. V. Lomonosov Moscow State University

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/40, Leninskie Gory, Moscow, 119992

P. Sergiev

A. N. Belozersky Research Institute of Physico-Chemical Biology, M. V. Lomonosov Moscow State University

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/40, Leninskie Gory, Moscow, 119992

R. Yamidanov

Institute of Biochemistry and Genetics, Ufa Scientific Center, Russian Academy of Sciences

Email: ekaterina.deyneka@phystech.edu
Rússia, 71 Prosp. Oktyabrya, Ufa, Republic of Bashkortostan, 450054

E. Deineka

Moscow Institute of Physics and Technology (State University)

Autor responsável pela correspondência
Email: ekaterina.deyneka@phystech.edu
Rússia, 9 Institutskii Pereul., Moscow Region, Dolgoprudnyi, 141700

V. Terent’ev

Institute of Biochemistry and Genetics, Ufa Scientific Center, Russian Academy of Sciences

Email: ekaterina.deyneka@phystech.edu
Rússia, 71 Prosp. Oktyabrya, Ufa, Republic of Bashkortostan, 450054

G. Fil’kov

Moscow Institute of Physics and Technology (State University)

Email: ekaterina.deyneka@phystech.edu
Rússia, 9 Institutskii Pereul., Moscow Region, Dolgoprudnyi, 141700

A. Sofronova

Department of Bioengineering and Bioinformatics, M. V. Lomonosov Moscow State University

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/73 Leninskie Gory, Moscow, 119234

A. Mazhuga

Department of Chemistry, M. V. Lomonosov Moscow State University; National University of Science and Technology Moscow Institute of Steel and Alloys (MISiS); D. I. Mendeleev University of Chemical Technology of Russia

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/3 Leninskie Gory, Moscow, 119991; 4 Leninskii Prosp., Moscow, 119049; 9 Miusskaya Sq., Moscow, 125047

O. Dontsova

A. N. Belozersky Research Institute of Physico-Chemical Biology, M. V. Lomonosov Moscow State University

Email: ekaterina.deyneka@phystech.edu
Rússia, 1/40, Leninskie Gory, Moscow, 119992

Arquivos suplementares

Arquivos suplementares
Ação
1. JATS XML

Declaração de direitos autorais © Springer Science+Business Media, LLC, part of Springer Nature, 2019