Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors

Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3 H-imidazo[5,1- f][1,2,4]triazin-4-ones and pyrazolopyrimi-dinones, isomeric imidazo[1,5- a][1,3,5]triazin-4(3 H)-ones (e.g., 30) were also shown to be potent and selective PDE inhibitor scaff...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-09, Vol.15 (17), p.3900-3907
Main Authors: Haning, Helmut, Niewöhner, Ulrich, Schenke, Thomas, Lampe, Thomas, Hillisch, Alexander, Bischoff, Erwin
Format: Article
Language:English
Subjects:
3',5'-Cyclic-GMP Phosphodiesterases - antagonists & inhibitors
Biological and medical sciences
Cyclic Nucleotide Phosphodiesterases, Type 5
Heterocycles
Heterocyclic Compounds - chemical synthesis
Heterocyclic Compounds - pharmacology
Inhibitory Concentration 50
Medical sciences
Miscellaneous
PDE5 inhibition
Pharmacology. Drug treatments
Structure-Activity Relationship
Substrate Specificity
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Summary:Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3 H-imidazo[5,1- f][1,2,4]triazin-4-ones and pyrazolopyrimi-dinones, isomeric imidazo[1,5- a][1,3,5]triazin-4(3 H)-ones (e.g., 30) 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. Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3 H-imidazo[5,1- f][1,2,4]triazin-4-ones and pyrazolopyrimidinones, isomeric imidazo[1,5- a][1,3,5]triazin-4(3 H)-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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.05.090