Title: Design and synthesis of bioactive 1,2-annulated adamantane derivatives
Authors: Zoidis, Grigoris ×
Tsotinis, Andrew
Kolocouris, Nicolas
Kelly, John M
Prathalingam, S Radhika
Naesens, Lieve
De Clercq, Erik #
Issue Date: Sep-2008
Publisher: Royal Society of Chemistry
Series Title: Organic & Biomolecular Chemistry vol:6 issue:17 pages:3177-3185
Abstract: Adamantanopyrrolidines , and , adamantanopyrrolidines and , adamantanoxazolone , adamantanopyrazolone , adamantanopyrazolothione and adamantanocyclopentanamine were synthesized and tested for anti-influenza A virus and trypanocidal activity. The stereoelectronic requirements for optimal antiviral and trypanocidal potency were investigated. Pyrrolidine proved to be the most active of the compounds tested against influenza A virus, being 4-fold more active than amantadine, equipotent to rimantadine and 19-fold more potent than ribavirin. Oxazolone showed significant trypanocidal activity against bloodstream forms of the African trypanosome, Trypanosoma brucei, being approximately 3 times more potent than rimantadine and almost 50-fold more active than amantadine.
ISSN: 1477-0520
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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