Synthesis of camphecene derivatives using click chemistry methodology and study of their antiviral activity.
Artyushin OI, Sharova EV, Vinogradova NM, Genkina GK, Moiseeva AA, Klemenkova ZS, Orshanskaya IR, Shtro AA, Kadyrova RA, Zarubaev VV, Yarovaya OI, Salakhutdinov NF, Brel VK.
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.