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

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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 languageEnglish
Pages (from-to)1257-1263
Number of pages7
JournalJournal of medicinal chemistry
Issue number7
StatePublished - Apr 6 2000


All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Molecular Medicine

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