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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
https://doi.org/10.1021/jm000081+
Copyright © 2000 American Chemical Society

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    Abstract

    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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