Journal of Antibiotics, volume 72, issue 11, pages 827-833
2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials
Ivanenkov Yan A
1, 2, 3, 4
,
Yamidanov Renat S.
1
,
Osterman Ilya A.
3, 5
,
Sergiev Petr V.
5, 6
,
Aladinskiy Vladimir A.
2
,
Terentiev Victor A.
1, 2
,
Veselov Mark S.
1, 2
,
Ayginin Andrey A.
1, 2
,
Komarova Katerina S.
5, 7
,
Sadovnikov Sergey V
1
,
Matniyazov Rustam
1
,
Sofronova Alina A.
7
,
Malyshev Alexander S.
8
,
Machulkin Alexey E.
3
,
Petrov Rostislav A.
3
,
Lukianov Dmitrii
5
,
Iarovenko Svetlana
5, 7
,
Bezrukov Dmitry S.
3, 5
,
Baymiev Andrey Kh.
1
,
Dontsova Olga A.
3, 5, 6
1
4
ChemDiv, San Diego, USA
|
Publication type: Journal Article
Publication date: 2019-07-29
Journal:
Journal of Antibiotics
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor: 3.3
ISSN: 00218820, 18811469
Drug Discovery
Pharmacology
Abstract
The present report describes our efforts to identify new structural classes of compounds having promising antibacterial activity using previously published double-reporter system pDualrep2. This semi-automated high-throughput screening (HTS) platform has been applied to perform a large-scale screen of a diverse small-molecule compound library. We have selected a set of more than 125,000 molecules and evaluated them for their antibacterial activity. On the basis of HTS results, eight compounds containing 2-pyrazol-1-yl-thiazole scaffold exhibited moderate-to-high activity against ΔTolC Escherichia coli. Minimum inhibitory concentration (MIC) values for these molecules were in the range of 0.037–8 μg ml−1. The most active compound 8 demonstrated high antibacterial potency (MIC = 0.037 μg ml−1), that significantly exceed that measured for erythromycin (MIC = 2.5 μg ml−1) and was comparable with the activity of levofloxacin (MIC = 0.016 μg ml−1). Unfortunately, this compound showed only moderate selectivity toward HEK293 eukaryotic cell line. On the contrary, compound 7 was less potent (MIC = 0.8 μg ml−1) but displayed only slight cytotoxicity. Thus, 2-pyrazol-1-yl-thiazoles can be considered as a valuable starting point for subsequent optimization and morphing.
Citations by journals
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1
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Bioorganic and Medicinal Chemistry Letters
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1 publication, 14.29%
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1 publication, 14.29%
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1 publication, 14.29%
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Russian Journal of General Chemistry
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1 publication, 14.29%
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Metabolites
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Metabolites
1 publication, 14.29%
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1
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Citations by publishers
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1
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Elsevier
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Elsevier
1 publication, 14.29%
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Future Medicine
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Future Medicine
1 publication, 14.29%
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Wiley
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Wiley
1 publication, 14.29%
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Pleiades Publishing
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Pleiades Publishing
1 publication, 14.29%
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Multidisciplinary Digital Publishing Institute (MDPI)
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Multidisciplinary Digital Publishing Institute (MDPI)
1 publication, 14.29%
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1
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- We do not take into account publications that without a DOI.
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Ivanenkov Y. A. et al. 2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials // Journal of Antibiotics. 2019. Vol. 72. No. 11. pp. 827-833.
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Ivanenkov Y. A., Yamidanov R. S., Osterman I. A., Sergiev P. V., Aladinskiy V. A., V. Aladinskaya A., Terentiev V. A., Veselov M. S., Ayginin A. A., Skvortsov D. A., Komarova K. S., Sadovnikov S. V., Matniyazov R., Sofronova A. A., Malyshev A. S., Machulkin A. E., Petrov R. A., Lukianov D., Iarovenko S., Bezrukov D. S., Baymiev A. K., Dontsova O. A. 2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials // Journal of Antibiotics. 2019. Vol. 72. No. 11. pp. 827-833.
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TY - JOUR
DO - 10.1038/s41429-019-0211-y
UR - https://doi.org/10.1038%2Fs41429-019-0211-y
TI - 2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials
T2 - Journal of Antibiotics
AU - Yamidanov, Renat S.
AU - Osterman, Ilya A.
AU - Sergiev, Petr V.
AU - Aladinskiy, Vladimir A.
AU - V. Aladinskaya, Anastasia
AU - Terentiev, Victor A.
AU - Veselov, Mark S.
AU - Ayginin, Andrey A.
AU - Skvortsov, Dmitry A.
AU - Komarova, Katerina S.
AU - Sadovnikov, Sergey V
AU - Matniyazov, Rustam
AU - Sofronova, Alina A.
AU - Malyshev, Alexander S.
AU - Machulkin, Alexey E.
AU - Petrov, Rostislav A.
AU - Lukianov, Dmitrii
AU - Iarovenko, Svetlana
AU - Bezrukov, Dmitry S.
AU - Baymiev, Andrey Kh.
AU - Dontsova, Olga A.
AU - Ivanenkov, Yan A
PY - 2019
DA - 2019/07/29 00:00:00
PB - Springer Nature
SP - 827-833
IS - 11
VL - 72
SN - 0021-8820
SN - 1881-1469
ER -
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@article{2019_Ivanenkov,
author = {Renat S. Yamidanov and Ilya A. Osterman and Petr V. Sergiev and Vladimir A. Aladinskiy and Anastasia V. Aladinskaya and Victor A. Terentiev and Mark S. Veselov and Andrey A. Ayginin and Dmitry A. Skvortsov and Katerina S. Komarova and Sergey V Sadovnikov and Rustam Matniyazov and Alina A. Sofronova and Alexander S. Malyshev and Alexey E. Machulkin and Rostislav A. Petrov and Dmitrii Lukianov and Svetlana Iarovenko and Dmitry S. Bezrukov and Andrey Kh. Baymiev and Olga A. Dontsova and Yan A Ivanenkov},
title = {2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials},
journal = {Journal of Antibiotics},
year = {2019},
volume = {72},
publisher = {Springer Nature},
month = {jul},
url = {https://doi.org/10.1038%2Fs41429-019-0211-y},
number = {11},
pages = {827--833},
doi = {10.1038/s41429-019-0211-y}
}
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Ivanenkov, Yan A., et al. “2-Pyrazol-1-yl-thiazole derivatives as novel highly potent antibacterials.” Journal of Antibiotics, vol. 72, no. 11, Jul. 2019, pp. 827-833. https://doi.org/10.1038%2Fs41429-019-0211-y.