Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors

…, T Schenke, T Lampe, A Hillisch, E Bischoff

Index: Haning, Helmut; Niewoehner, Ulrich; Schenke, Thomas; Lampe, Thomas; Hillisch, Alexander; Bischoff, Erwin Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3900 - 3907

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Citation Number: 31

Abstract

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.