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Title: Synthesis of camphecene derivatives using click chemistry methodology and study of their antiviral activity
Authors: Artyushin, Oleg I
Sharova, Elena V
Vinogradova, Natalya M
Genkina, Galina K
Moiseeva, Aleksandra A
Klemenkova, Zinaida S
Orshanskaya, Iana R
Shtro, Anna A
Kadyrova, Renata A
Yarovaya, Olga I
Salakhutdinov, Nariman F
Brel, Valery K
Zarubaev, Vladimir V. 
Keywords: Acetylenes;Antivirals;Azides;Camphor;Click chemistry;Imine derivatives;Influenza;Triazoles
Issue Date: 2017
Publisher: Elsevier
Journal: Bioorganic and Medicinal Chemistry Letters 
Abstract: A series of seventeen tetrazole derivatives of 1,7,7-trimethyl-[2.2.1]bicycloheptane were synthesized using click chemistry methodology and characterized by spectral data. Studies of cytotoxicity and in vitro antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1) in MDCK cells of the compounds obtained were performed. The structure-activity relationship analysis suggests that to possess virus-inhibiting activity, the compounds of this group should bear oxygen atom with a short linker (C2-C4), either as a hydroxyl group (18, 19, 29), keto-group (21) or as a part of a heterocycle (24). These compounds demonstrated low cytotoxicity along with high anti-viral activity.
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2017.03.051
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