Literature DB >> 17337182

Potent and selective xanthine-based inhibitors of phosphodiesterase 5.

Nichola J Arnold1, 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.   

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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Year:  2006        PMID: 17337182     DOI: 10.1016/j.bmcl.2006.11.019

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Investigation of PDE5/PDE6 and PDE5/PDE11 selective potent tadalafil-like PDE5 inhibitors using combination of molecular modeling approaches, molecular fingerprint-based virtual screening protocols and structure-based pharmacophore development.

Authors:  Gülru Kayık; Nurcan Ş Tüzün; Serdar Durdagi
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

  1 in total

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