Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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. и др.
в: MedChemComm, Том 8, № 5, 01.05.2017, стр. 960-963.Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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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