Molecular Diversity, том 24, издание 1, номера страниц: 233-239

Identification of pyrrolo-pyridine derivatives as novel class of antibacterials

Veselov Mark S. 1, 2, 3
Ivanenkov Yan A. 1, 2, 3, 4, 5
Yamidanov Renat S. 1
Osterman Ilya A. 3, 4
Sergiev Petr V. 3, 6
Aladinskiy Vladimir A. 2, 3
Aladinskaya Anastasia V. 2, 3
Terentiev Victor A. 1, 2, 3
Ayginin Andrey A. 1, 2
Chemeris Alexey V. 1
Baimiev Alexey Kh. 1
Sofronova Alina A. 7
Machulkin Alexey E. 4
Petrov Rostislav A. 4
Maklakova Svetlana Yu. 4
Bezrukov Dmitry S. 3
Filkov Gleb I. 2
Zainullina Liana F. 1
Maximova Marina A. 1
Zileeva Zulfiya R. 1
Kartsev Victor G. 8
Vakhitova Yulia V. 1
Тип документаJournal Article
Дата публикации2019-04-04
ИздательSpringer Nature
Название журналаMolecular Diversity
Квартиль по SCImagoQ3
Квартиль по Web of ScienceQ2
Импакт-фактор 20213.36
ISSN13811991, 1573501X
Catalysis
Organic Chemistry
Drug Discovery
Inorganic Chemistry
Physical and Theoretical Chemistry
Molecular Biology
General Medicine
Information Systems
Краткое описание
Abstract A series of 5-oxo-4 H -pyrrolo[3,2-b]pyridine derivatives was identified as novel class of highly potent antibacterial agents during an extensive large-scale high-throughput screening (HTS) program utilizing a unique double-reporter system—pDualrep2. The construction of the reporter system allows us to perform visual inspection of the underlying mechanism of action due to two genes—Katushka2S and RFP—which encode the proteins with different imaging signatures. Antibacterial activity of the compounds was evaluated during the initial HTS round and subsequent rescreen procedure. The most active molecule demonstrated a MIC value of 3.35 µg/mL against E. coli with some signs of translation blockage (low Katushka2S signal) and no SOS response. The compound did not demonstrate cytotoxicity in standard cell viability assay. Subsequent structural morphing and follow-up synthesis may result in novel compounds with a meaningful antibacterial potency which can be reasonably regarded as an attractive starting point for further in vivo investigation and optimization. Graphical abstract
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1. Veselov M.S. и др. Identification of pyrrolo-pyridine derivatives as novel class of antibacterials // Molecular Diversity. 2019. Т. 24. № 1. С. 233–239.
RIS |
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TY - JOUR

DO - 10.1007/s11030-019-09946-3

UR - http://dx.doi.org/10.1007/s11030-019-09946-3

TI - Identification of pyrrolo-pyridine derivatives as novel class of antibacterials

T2 - Molecular Diversity

AU - Veselov, Mark S.

AU - Ivanenkov, Yan A.

AU - Yamidanov, Renat S.

AU - Osterman, Ilya A.

AU - Sergiev, Petr V.

AU - Aladinskiy, Vladimir A.

AU - Aladinskaya, Anastasia V.

AU - Terentiev, Victor A.

AU - Ayginin, Andrey A.

AU - Skvortsov, Dmitry A.

AU - Komarova, Katerina S.

AU - Chemeris, Alexey V.

AU - Baimiev, Alexey Kh.

AU - Sofronova, Alina A.

AU - Machulkin, Alexey E.

AU - Petrov, Rostislav A.

AU - Maklakova, Svetlana Yu.

AU - Bezrukov, Dmitry S.

AU - Filkov, Gleb I.

AU - Zainullina, Liana F.

AU - Maximova, Marina A.

AU - Zileeva, Zulfiya R.

AU - Kartsev, Victor G.

AU - Vakhitova, Yulia V.

AU - Dontsova, Olga A.

PY - 2019

DA - 2019/04/04

PB - Springer Science and Business Media LLC

SP - 233-239

IS - 1

VL - 24

SN - 1381-1991

SN - 1573-501X

ER -

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@article{2019,

doi = {10.1007/s11030-019-09946-3},

url = {https://doi.org/10.1007%2Fs11030-019-09946-3},

year = 2019,

month = {apr},

publisher = {Springer Science and Business Media {LLC}},

volume = {24},

number = {1},

pages = {233--239},

author = {Mark S. Veselov and Yan A. Ivanenkov and Renat S. Yamidanov and Ilya A. Osterman and Petr V. Sergiev and Vladimir A. Aladinskiy and Anastasia V. Aladinskaya and Victor A. Terentiev and Andrey A. Ayginin and Dmitry A. Skvortsov and Katerina S. Komarova and Alexey V. Chemeris and Alexey Kh. Baimiev and Alina A. Sofronova and Alexey E. Machulkin and Rostislav A. Petrov and Svetlana Yu. Maklakova and Dmitry S. Bezrukov and Gleb I. Filkov and Liana F. Zainullina and Marina A. Maximova and Zulfiya R. Zileeva and Victor G. Kartsev and Yulia V. Vakhitova and Olga A. Dontsova},

title = {Identification of pyrrolo-pyridine derivatives as novel class of antibacterials}

}

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Veselov, Mark S. et al. “Identification of Pyrrolo-Pyridine Derivatives as Novel Class of Antibacterials.” Molecular Diversity 24.1 (2019): 233–239. Crossref. Web.