Potent and selective xanthine-based inhibitors of phosphodiesterase 5

  • Bioorg Med Chem Lett. 2007 Apr 15;17(8):2376-9. doi: 10.1016/j.bmcl.2006.11.019.
Nichola J Arnold  1 ,  Ruth Arnold ,  David Beer ,  Gurdip Bhalay ,  Stephen P Collingwood ,  Sarah Craig ,  Nicholas Devereux ,  Mark Dodds ,  Andrew R Dunstan ,  Robin A Fairhurst ,  David Farr ,  Joseph D Fullerton ,  Angela Glen ,  Sylvie Gomez ,  Sandra Haberthuer ,  Julia D I Hatto ,  Colin Howes ,  Darryl Jones ,  Thomas H Keller ,  Beate Leuenberger ,  Heinz E Moser ,  Irene Muller ,  Reto Naef ,  Paul A Nicklin ,  David A Sandham ,  Katharine L Turner ,  Morris F Tweed ,  Simon J Watson ,  Mauro Zurini
Affiliations
  • 1. Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
PMID: 17337182 DOI: 10.1016/j.bmcl.2006.11.019
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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