New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
A series of potent PDE5 inhibitors with high selectivity versus PDE6 isoenzymes was identified.
Feixas
Joan
J
Almirall Prodesfarma Research Center, Cardener 68-74, 08024 Barcelona, Spain.
Giovannoni
Maria Paola
MP
Vergelli
Claudia
C
Gavaldà
Amadeu
A
Cesari
Nicoletta
N
Graziano
Alessia
A
Dal Piaz
Vittorio
V
D015106:3',5'-Cyclic-GMP Phosphodiesterases; D000818:Animals; D001792:Blood Platelets / Q000201:enzymology; D002417:Cattle; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D054707:Cyclic Nucleotide Phosphodiesterases, Type 6; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000097:blood / Q000378:metabolism*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012160:Retina / Q000201:enzymology; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
D010726:Phosphodiesterase Inhibitors; D011720:Pyrazoles; D011724:Pyridazines; D010727:Phosphoric Diester Hydrolases; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D054707:Cyclic Nucleotide Phosphodiesterases, Type 6