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.
Original language | English |
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Pages (from-to) | 2181-2184 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 27 |
Issue number | 10 |
DOIs | |
Publication status | Published - 15 May 2017 |
Keywords
- Acetylenes
- Antivirals
- Azides
- Camphor
- Click chemistry
- Imine derivatives
- Influenza
- Triazoles
- AZIDE-ALKYNE CYCLOADDITION
- DESIGN
- DISCOVERY
- 1,2,3-TRIAZOLES
- INHIBITORS
- INFLUENZA-VIRUS ENTRY
- Antiviral Agents/chemical synthesis
- Click Chemistry
- Humans
- Structure-Activity Relationship
- Ethanolamines/chemical synthesis
- Animals
- Influenza A Virus, H1N1 Subtype/drug effects
- Camphor/analogs & derivatives
- Dogs
- Madin Darby Canine Kidney Cells