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

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

  • Bioorg Med Chem Lett. 2002 Mar 25;12(6):865-8. doi: 10.1016/s0960-894x(02)00030-6.
Helmut Haning 1,  Ulrich Niewöhner,  Thomas Schenke,  Mazen Es-Sayed,  Gunter Schmidt,  Thomas Lampe,  Erwin Bischoff
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, BAYER AG, Business Group Pharma, D-42096, Wuppertal, Germany. helmut.haning.b@bayer.com
PMID: 11958981 DOI: 10.1016/s0960-894x(02)00030-6
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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