title: Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.
abstract: 2-aryl-substituted imidazo[5,1-f][1,2,4]triazin-4(3H)-ones represent a new class of potent cGMP-PDE 5 inhibitors that prove to be superior to other purine-isosteric inhibitors. Subnanomolar inhibitors of PDE 5 with activity in in vivo models for erectile dysfunction have been identified. BAY 38-9456 (Vardenafil-hydrochloride) has been selected for clinical studies in the indication of erectile dysfunction.
authors.affiliation: Department of Medicinal Chemistry, BAYER AG, Business Group Pharma, D-42096, Wuppertal, Germany. helmut.haning.b@bayer.com
authors.forename: Helmut
authors.initials: H
authors.lastname: Haning
authors.forename: Ulrich
authors.initials: U
authors.lastname: Niewöhner
authors.forename: Thomas
authors.initials: T
authors.lastname: Schenke
authors.forename: Mazen
authors.initials: M
authors.lastname: Es-Sayed
authors.forename: Gunter
authors.initials: G
authors.lastname: Schmidt
authors.forename: Thomas
authors.initials: T
authors.lastname: Lampe
authors.forename: Erwin
authors.initials: E
authors.lastname: Bischoff
mesh_terms: D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000818:Animals; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D007172:Erectile Dysfunction / Q000188:drug therapy; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008297:Male; D011485:Protein Binding; D011817:Rabbits; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D007093:Imidazoles; D014227:Triazines; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5