Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors
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摘要:
2-aryl-substituted imidazo[5,1-][1,2,4]triazin-4(3)-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.2-aryl substituted imidazo[5,1-][1,2,4]triazin-4(3)-ones represent a new class of potent cGMP-PDE inhibitors which proves to be superior to other purine-isosteric inhibitors. Subnanomolar and orally bioavailable inhibitors of PDE 5 have been identified. BAY 38-9456 (Vardenafil* HCl) is currently being evaluated in clinical studies for the indication erectile dysfunction.
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DOI:
10.1016/S0960-894X(02)00030-6
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年份:
2002
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