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Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus. / Sokolova, A. S.; Yarovaya, O. I.; Semenova, M. D. et al.

In: MedChemComm, Vol. 8, No. 5, 01.05.2017, p. 960-963.

Research output: Contribution to journal › Article › peer-review

Harvard

Sokolova, AS, Yarovaya, OI, Semenova, MD, Shtro, AA, Orshanskaya, IR, Zarubaev, VV & Salakhutdinov, NF 2017, 'Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus', MedChemComm, vol. 8, no. 5, pp. 960-963. https://doi.org/10.1039/c6md00657d

APA

Sokolova, A. S., Yarovaya, O. I., Semenova, M. D., Shtro, A. A., Orshanskaya, I. R., Zarubaev, V. V., & Salakhutdinov, N. F. (2017). Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus. MedChemComm, 8(5), 960-963. https://doi.org/10.1039/c6md00657d

Vancouver

Sokolova AS, Yarovaya OI, Semenova MD, Shtro AA, Orshanskaya IR, Zarubaev VV et al. Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus. MedChemComm. 2017 May 1;8(5):960-963. doi: 10.1039/c6md00657d

Author

Sokolova, A. S. ; Yarovaya, O. I. ; Semenova, M. D. et al. / Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus. In: MedChemComm. 2017 ; Vol. 8, No. 5. pp. 960-963.

BibTeX

@article{003a5ea324464a148620d21e1a604467,
title = "Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus",
abstract = "Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.",
keywords = "CHANNEL, DISCOVERY, OSELTAMIVIR-RESISTANT INFLUENZA, UNITED-STATES, VIVO",
author = "Sokolova, {A. S.} and Yarovaya, {O. I.} and Semenova, {M. D.} and Shtro, {A. A.} and Orshanskaya, {I. R.} and Zarubaev, {V. V.} and Salakhutdinov, {N. F.}",
year = "2017",
month = may,
day = "1",
doi = "10.1039/c6md00657d",
language = "English",
volume = "8",
pages = "960--963",
journal = "MedChemComm",
issn = "2040-2503",
publisher = "Royal Society of Chemistry",
number = "5",

}

RIS

TY - JOUR

T1 - Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus

AU - Sokolova, A. S.

AU - Yarovaya, O. I.

AU - Semenova, M. D.

AU - Shtro, A. A.

AU - Orshanskaya, I. R.

AU - Zarubaev, V. V.

AU - Salakhutdinov, N. F.

PY - 2017/5/1

Y1 - 2017/5/1

N2 - Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.

AB - Herein, we present the design and synthesis of a series of novel heterocyclic derivatives of (-)-borneol and (-)-isoborneol as potent inhibitors of the influenza A virus. All compounds were tested for their toxicity against MDCK cells and for virus-inhibiting activity against the influenza virus A/Puerto Rico/8/34 (H1N1). Compounds 7, 16 and 26 containing a morpholine fragment exhibited the highest efficiency as agents inhibiting the replication of the influenza virus A(H1N1) with selectivity indices of 82, 45 and 65, correspondingly. Derivatives 9 (SI = 23) and 18 (SI = 25) containing a 1-methylpiperazine motif showed moderate antiviral activity. Structure-activity analysis of this new series of borneol derivatives revealed that a 1,7,7-trimethylbicyclo[2.2.1]heptan scaffold is required for the antiviral activity.

KW - CHANNEL

KW - DISCOVERY

KW - OSELTAMIVIR-RESISTANT INFLUENZA

KW - UNITED-STATES

KW - VIVO

UR - http://www.scopus.com/inward/record.url?scp=85021957010&partnerID=8YFLogxK

U2 - 10.1039/c6md00657d

DO - 10.1039/c6md00657d

M3 - Article

C2 - 30108810

AN - SCOPUS:85021957010

VL - 8

SP - 960

EP - 963

JO - MedChemComm

JF - MedChemComm

SN - 2040-2503

IS - 5

ER -

ID: 9561058