Aliphatic and alicyclic camphor imines as effective inhibitors of influenza virus H1N1

作者：Sokolova Anastasiya S; Yarovaya Olga I^*; Baev Dmitry S; Shernyukov Andrey V; Shtro Anna A; Zarubaev Vladimir V^*; Salakhutdinov Nariman F

来源：European Journal of Medicinal Chemistry, 2017, 127: 661-670.

DOI：10.1016/j.ejmech.2016.10.035

• Influenza
• Camphor derivatives
• Antiviral
• Cage compounds

A series of camphor derived imines was synthesised and evaluated in vitro for antiviral activity. Theoretical evaluations of ADME properties were also carried out. Most of these compounds exhibited significant activity against the drug-resistant strains of influenza A virus. Especially, compounds 2 (SI = 632) and 3 (SI = 417) presented high inhibition against influenza subtypes A/Puerto Rico/8/34 and A/California/07/09 of H1N1pdm09. Analysis of the structure-activity relationship showed that the activity was strongly dependent on the length of the aliphatic chain: derivatives with a shorter chain possessed higher activity, while the suppressing action of compounds with long aliphatic chains was lower.

• 出版日期2017-2-15