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Potent and selective xanthine-based inhibitors of phosphodiesterase 5
Authors:Arnold Nichola J  Arnold Ruth  Beer David  Bhalay Gurdip  Collingwood Stephen P  Craig Sarah  Devereux Nicholas  Dodds Mark  Dunstan Andrew R  Fairhurst Robin A  Farr David  Fullerton Joseph D  Glen Angela  Gomez Sylvie  Haberthuer Sandra  Hatto Julia D I  Howes Colin  Jones Darryl  Keller Thomas H  Leuenberger Beate  Moser Heinz E  Muller Irene  Naef Reto  Nicklin Paul A  Sandham David A  Turner Katharine L  Tweed Morris F  Watson Simon J  Zurini Mauro
Affiliation:Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
Abstract:Inhibitors of PDE5 are useful therapeutic agents for treatment of erectile dysfunction. A series of novel xanthine derivatives has been identified as potent inhibitors of PDE5, with good levels of selectivity against other PDE isoforms, including PDE6. Studies in the dog indicate excellent oral bioavailability for compound 21.
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