Title: Design and synthesis of 1,2-annulated adamantane piperidines with anti-influenza virus activity
Authors: Zoidis, Grigoris ×
Kolocouris, Nicolas
Naesens, Lieve
De Clercq, Erik #
Issue Date: Feb-2009
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:17 issue:4 pages:1534-1541
Abstract: 1-2 Annulated adamantane piperidines 4, 6, 16, 17, 19, 23 and 25 were synthesized and evaluated for anti-influenza A virus activity. The stereoelectronic requirements for optimal antiviral potency were investigated. Piperidine 23 proved to be the most active of the compounds tested against influenza A virus, being 3.5-fold more active than amantadine, equipotent to rimantadine and 15-fold more potent than ribavirin. It is noteworthy that piperidine 23 displayed one of the highest selectivity indexes (SI>732) among aminoadamantanes or other cage structure amines tested till now.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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