N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction

David P. Rotella; Zhong Sun; Yeheng Zhu; John Krupinski; Ronald Pongrac; Laurie Seliger; Diane Normandin; John E. Macor

doi:10.1021/jm000081+

N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction

David P. Rotella, Zhong Sun, Yeheng Zhu, John Krupinski, Ronald Pongrac, Laurie Seliger, Diane Normandin, John E. Macor

Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

55 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	1257-1263
Number of pages	7
Journal	Journal of Medicinal Chemistry
Volume	43
Issue number	7
DOIs	https://doi.org/10.1021/jm000081+
State	Published - 6 Apr 2000

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abstract = "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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AU - Rotella, David P.

AU - Sun, Zhong

AU - Zhu, Yeheng

AU - Krupinski, John

AU - Pongrac, Ronald

AU - Seliger, Laurie

AU - Normandin, Diane

AU - Macor, John E.

PY - 2000/4/6

Y1 - 2000/4/6

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AB - 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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ER -

N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction

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