Dp. Rotella et al., N-3-substituted imidazoquinazolinones: Potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction, J MED CHEM, 43(7), 2000, pp. 1257-1263
Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme select
ivity relative to sildenafil may result in agents for the treatment of male
erectile dysfunction (MED) with a lower incidence of PDE-associated advers
e effects. This paper describes the discovery of 14, a PDE5 inhibitor with
improved potency and selectivity in vitro compared to sildenafil. This comp
ound shows activity in a functional assay of erectile function comparable t
o that of sildenafil.