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

…, Y Zhu, J Krupinski, R Pongrac, L Seliger…

文献索引：Rotella, David P.; Sun, Zhong; Zhu, Yeheng; Krupinski, John; Pongrac, Ronald; Seliger, Laurie; Normandin, Diane; Macor, John E. Journal of Medicinal Chemistry, 2000 , vol. 43, # 7 p. 1257 - 1263

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被引用次数: 58

摘要

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 ...