Combinatorial Chemistry and High Throughput Screening, volume 22, issue 6, pages 400-410

Substituted furanocoumarins as novel class of antibacterial translation inhibitors

Ivanenkov Yan A 1
Yamidanov Renat S. 1
Ayginin Andrey A. 1
Aladinskiy Vladimir A. 3
Aladinskaya Anastasia V. 3
Terentiev Victor A. 1
Veselov Mark S. 1
Chemeris Alexey V. 1
Zainullina Liana F. 1
Maximova Marina A. 1
Zileeva Zulfiya R. 1
Vakhitova Yulia V. 1
Baymiev Alexey Kh. 1
Baymiev Andrey Kh. 1
Sofronova Alina A. 5
Machulkin Alexey E. 6
Petrov Rostislav A. 6
Bezrukov Dmitry S. 6
Puchinina Maria M. 3
Publication typeJournal Article
Publication date2019-09-05
Quartile SCImago
Q3
Quartile WOS
Q3
Impact factor1.8
ISSN13862073, 18755402
Organic Chemistry
Drug Discovery
Computer Science Applications
General Medicine
Abstract
Introduction:

A variety of organic compounds has been reported to have antibacterial activity. However, antimicrobial resistance is one of the main problems of current anti-infective therapy, and the development of novel antibacterials is one of the main challenges of current drug discovery.

Methods:

Using our previously developed dual-reporter High-Throughput Screening (HTS) platform, we identified a series of furanocoumarins as having high antibacterial activity. The construction of the reporter system allows us to differentiate three mechanisms of action for the active compounds: inhibition of protein synthesis (induction of Katushka2S), DNA damaging (induction of RFP) or other (inhibition of bacterial growth without reporter induction).

Results:

Two primary hit-molecules of furanocoumarin series demonstrated relatively low MIC values comparable to that observed for Erythromycin (Ery) against E. coli and weakly induced both reporters. Dose-dependent translation inhibition was shown using in vitro luciferase assay, however it was not confirmed using C14-test. A series of close structure analogs of the identified hits was obtained and investigated using the same screening platform. Compound 19 was found to have slightly lower MIC value (15.18 µM) and higher induction of Katushka2S reporter in contrast to the parent structures. Moreover, translation blockage was clearly identified using both in vitro luciferase assay and C14 test. The standard cytotoxicity test revealed a relatively low cytotoxicity of the most active molecules.

Conclusion:

High antibacterial activity in combination with low cytotoxicity was demonstrated for a series of furanocoumarins. Further optimization of the described structures may result in novel and attractive lead compounds with promising antibacterial efficiency.

Citations by journals

1
Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters, 1, 100%
Bioorganic and Medicinal Chemistry Letters
1 publication, 100%
1

Citations by publishers

1
Elsevier
Elsevier, 1, 100%
Elsevier
1 publication, 100%
1
  • We do not take into account publications that without a DOI.
  • Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
  • Statistics recalculated weekly.
Metrics
Share
Cite this
GOST |
Cite this
GOST Copy
Ivanenkov Y. A. et al. Substituted furanocoumarins as novel class of antibacterial translation inhibitors // Combinatorial Chemistry and High Throughput Screening. 2019. Vol. 22. No. 6. pp. 400-410.
GOST all authors (up to 50) Copy
Ivanenkov Y. A., Yamidanov R. S., Osterman I. A., Sergiev P. V., Ayginin A. A., Aladinskiy V. A., Aladinskaya A. V., Terentiev V. A., Veselov M. S., Skvortsov D. A., Komarova K. S., Chemeris A. V., Zainullina L. F., Maximova M. A., Zileeva Z. R., Vakhitova Y. V., Baymiev A. K., Baymiev A. K., Sofronova A. A., Machulkin A. E., Petrov R. A., Bezrukov D. S., Puchinina M. M., Lukianov D. A., Dontsova O. A. Substituted furanocoumarins as novel class of antibacterial translation inhibitors // Combinatorial Chemistry and High Throughput Screening. 2019. Vol. 22. No. 6. pp. 400-410.
RIS |
Cite this
RIS Copy
TY - JOUR
DO - 10.2174/1386207322666190723110539
UR - https://doi.org/10.2174%2F1386207322666190723110539
TI - Substituted furanocoumarins as novel class of antibacterial translation inhibitors
T2 - Combinatorial Chemistry and High Throughput Screening
AU - Ivanenkov, Yan A
AU - Yamidanov, Renat S.
AU - Osterman, Ilya A.
AU - Sergiev, Petr V.
AU - Ayginin, Andrey A.
AU - Aladinskiy, Vladimir A.
AU - Aladinskaya, Anastasia V.
AU - Terentiev, Victor A.
AU - Veselov, Mark S.
AU - Skvortsov, Dmitry A.
AU - Komarova, Katerina S.
AU - Chemeris, Alexey V.
AU - Zainullina, Liana F.
AU - Maximova, Marina A.
AU - Zileeva, Zulfiya R.
AU - Vakhitova, Yulia V.
AU - Baymiev, Alexey Kh.
AU - Baymiev, Andrey Kh.
AU - Sofronova, Alina A.
AU - Machulkin, Alexey E.
AU - Petrov, Rostislav A.
AU - Bezrukov, Dmitry S.
AU - Puchinina, Maria M.
AU - Lukianov, Dmitrii A.
AU - Dontsova, Olga A.
PY - 2019
DA - 2019/09/05 00:00:00
PB - Bentham Science
SP - 400-410
IS - 6
VL - 22
SN - 1386-2073
SN - 1875-5402
ER -
BibTex |
Cite this
BibTex Copy
@article{2019_Ivanenkov
author = {Yan A Ivanenkov and Renat S. Yamidanov and Ilya A. Osterman and Petr V. Sergiev and Andrey A. Ayginin and Vladimir A. Aladinskiy and Anastasia V. Aladinskaya and Victor A. Terentiev and Mark S. Veselov and Dmitry A. Skvortsov and Katerina S. Komarova and Alexey V. Chemeris and Liana F. Zainullina and Marina A. Maximova and Zulfiya R. Zileeva and Yulia V. Vakhitova and Alexey Kh. Baymiev and Andrey Kh. Baymiev and Alina A. Sofronova and Alexey E. Machulkin and Rostislav A. Petrov and Dmitry S. Bezrukov and Maria M. Puchinina and Dmitrii A. Lukianov and Olga A. Dontsova},
title = {Substituted furanocoumarins as novel class of antibacterial translation inhibitors},
journal = {Combinatorial Chemistry and High Throughput Screening},
year = {2019},
volume = {22},
publisher = {Bentham Science},
month = {sep},
url = {https://doi.org/10.2174%2F1386207322666190723110539},
number = {6},
pages = {400--410},
doi = {10.2174/1386207322666190723110539}
}
MLA
Cite this
MLA Copy
Ivanenkov, Yan A., et al. “Substituted furanocoumarins as novel class of antibacterial translation inhibitors.” Combinatorial Chemistry and High Throughput Screening, vol. 22, no. 6, Sep. 2019, pp. 400-410. https://doi.org/10.2174%2F1386207322666190723110539.
Found error?