Imidazo[5,1- f ] [1,2,4] triazin-4(3 H )-ones, a new class of potent PDE 5 inhibitors

Bioorganic & Medicinal Chemistry Letters
2002.0

Abstract

2-aryl-substituted imidazo[5,1-f][1,2,4]triazin-4(3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.

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