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Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

Bioorganic & medicinal chemistry letters 2005 Sep 1; 15(17):3900-7

Link to PubMed abstract

Haning H H, Niewöhner U U, Schenke T T, Lampe T T, Hillisch A A, Bischoff E E

BAYER HealthCare AG, Business Group Pharma, D-42096 Wuppertal, Germany. helmut.Haning@bayerhealthcare.com

Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3H-imidazo[5,1-f][1,2,4]triazin-4-ones and pyrazolopyrimidinones, isomeric imidazo[1,5-a][1,3,5]triazin-4(3H)-ones were also shown to be potent and selective PDE inhibitor scaffolds with in vivo activity. SAR trends were elucidated for sulfonamide derivatives with generality across different scaffolds.