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 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.
BAYER HealthCare AG, Business Group Pharma, D-42096 Wuppertal, Germany. helmut.Haning@bayerhealthcare.com
Helmut
H
Haning
Ulrich
U
Niewöhner
Thomas
T
Schenke
Thomas
T
Lampe
Alexander
A
Hillisch
Erwin
E
Bischoff
D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D006571:Heterocyclic Compounds; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5