Comparison of different heterocyclic scaffolds as ...[Bioorg Med Chem Lett. 2005]

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1: Bioorg Med Chem Lett. 2005 Sep 1;15(17):3900-7. Links

Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

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

PMID: 15993055 [PubMed - indexed for MEDLINE]

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Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

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