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Title: Synthesis and in vitro study of novel borneol derivatives as potent inhibitors of the influenza A virus
Authors: Sokolova, A S
Yarovaya, O I
Semenova, M D
Shtro, A A
Orshanskaya, I R
Salakhutdinov, N F
Zarubaev, Vladimir V. 
Issue Date: 1-May-2017
Publisher: Royal Society of Chemistry
Journal: MedChemComm 
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.
ISSN: 2040-2503
DOI: 10.1039/c6md00657d
Appears in Collections:Journal articles

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