Molecular Diversity, издание 24, том 1, страницы 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.
2, 4
,
Sergiev Petr V.
2, 6
,
Aladinskiy Vladimir A.
2, 3
,
Aladinskaya Anastasia V.
2, 3
,
Terentiev Victor A.
1, 2, 3
,
Ayginin Andrey A.
1, 3
,
Komarova Katerina S.
2, 6
,
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.
2
,
Filkov Gleb I.
3
,
Zainullina Liana F.
1
,
Maximova Marina A.
1
,
Zileeva Zulfiya R.
1
,
Kartsev Victor G.
8
,
Vakhitova Yulia V.
1
,
Dontsova Olga A.
2, 4, 6
1
3
5
ChemDiv, San Diego, USA
8
InterBioScreen Ltd, Chernogolovka, Russian Federation
Тип публикации: Journal Article
Дата публикации: 2019-04-04
Springer Nature
Журнал:
Molecular Diversity
Квартиль SCImago: Q2
Квартиль WOS: Q2
Impact factor: 3.8
ISSN: 13811991, 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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Bioorganic and Medicinal Chemistry Letters
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Critical Reviews in Analytical Chemistry
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Veselov M. S. et al. Identification of pyrrolo-pyridine derivatives as novel class of antibacterials // Molecular Diversity. 2019. Vol. 24. No. 1. pp. 233-239.
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Veselov M. S., Ivanenkov Y. A., Yamidanov R. S., Osterman I. A., Sergiev P. V., Aladinskiy V. A., Aladinskaya A. V., Terentiev V. A., Ayginin A. A., Skvortsov D. A., Komarova K. S., Chemeris A. V., Baimiev A. K., Sofronova A. A., Machulkin A. E., Petrov R. A., Maklakova S. Yu., Bezrukov D. S., Filkov G. I., Zainullina L. F., Maximova M. A., Zileeva Z. R., Kartsev V. G., Vakhitova Y. V., Dontsova O. A. Identification of pyrrolo-pyridine derivatives as novel class of antibacterials // Molecular Diversity. 2019. Vol. 24. No. 1. pp. 233-239.
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TY - JOUR
DO - 10.1007/s11030-019-09946-3
UR - https://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 - Yamidanov, Renat S.
AU - Osterman, Ilya A.
AU - Sergiev, Petr V.
AU - Aladinskiy, Vladimir A.
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 - Bezrukov, Dmitry S.
AU - Filkov, Gleb I.
AU - Maximova, Marina A.
AU - Zileeva, Zulfiya R.
AU - Kartsev, Victor G.
AU - Vakhitova, Yulia V.
AU - Dontsova, Olga A.
AU - Ivanenkov, Yan A
AU - Aladinskaya, Anastasia V.
AU - Maklakova, Svetlana Yu
AU - Zainullina, Liana F.
PY - 2019
DA - 2019/04/04 00:00:00
PB - Springer Nature
SP - 233-239
IS - 1
VL - 24
SN - 1381-1991
SN - 1573-501X
ER -
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@article{2019_Veselov
author = {Mark S. Veselov and Renat S. Yamidanov and Ilya A. Osterman and Petr V. Sergiev and Vladimir A. Aladinskiy 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 Dmitry S. Bezrukov and Gleb I. Filkov and Marina A. Maximova and Zulfiya R. Zileeva and Victor G. Kartsev and Yulia V. Vakhitova and Olga A. Dontsova and Yan A Ivanenkov and Anastasia V. Aladinskaya and Svetlana Yu Maklakova and Liana F. Zainullina},
title = {Identification of pyrrolo-pyridine derivatives as novel class of antibacterials},
journal = {Molecular Diversity},
year = {2019},
volume = {24},
publisher = {Springer Nature},
month = {apr},
url = {https://doi.org/10.1007/s11030-019-09946-3},
number = {1},
pages = {233--239},
doi = {10.1007/s11030-019-09946-3}
}
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Veselov, Mark S., et al. “Identification of pyrrolo-pyridine derivatives as novel class of antibacterials.” Molecular Diversity, vol. 24, no. 1, Apr. 2019, pp. 233-239. https://doi.org/10.1007/s11030-019-09946-3.