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N-3-Substituted Imidazoquinazolinones:  Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile Dysfunction

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Discovery Chemistry and Cardiovascular Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, P.O. Box 5400, Princeton, New Jersey 08543-5400
Cite this: J. Med. Chem. 2000, 43, 7, 1257–1263
Publication Date (Web):March 18, 2000
Copyright © 2000 American Chemical Society

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    Abstract Image

    Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile dysfunction (MED) with a lower incidence of PDE-associated adverse effects. This paper describes the discovery of 14, a PDE5 inhibitor with improved potency and selectivity in vitro compared to sildenafil. This compound shows activity in a functional assay of erectile function comparable to that of sildenafil.

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     Corresponding author:  David P. Rotella. Phone:  609-818-5398. Fax:  609-818-3450. E-mail:  [email protected].

     Discovery Chemistry.


     Cardiovascular Drug Discovery.

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    32. David P. Rotella. Phosphodiesterase 5 inhibitors: current status and potential applications. Nature Reviews Drug Discovery 2002, 1 (9) , 674-682.
    33. Gerald B. Brock, Derek Bochinski. Modern pharmacotherapy for erectile dysfunction: evolving concepts with central and peripheral acting agents. Current Opinion in Urology 2001, 11 (6) , 625-630.
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