bay-73-6691 and Dementia--Vascular

bay-73-6691 has been researched along with Dementia--Vascular* in 1 studies

Other Studies

1 other study(ies) available for bay-73-6691 and Dementia--Vascular

Article	Year
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia. Journal of medicinal chemistry, 2019, 04-25, Volume: 62, Issue:8 To identify phosphodiesterase-9 (PDE9) as a novel target for the treatment of vascular dementia (VaD), a series of pyrazolopyrimidinone analogues were discovered based on a hit 1. Hit-to-lead optimization resulted in a potent inhibitor 2 with excellent selectivity and physicochemical properties to enable in vivo studies. Oral administration of 2 (5.0 mg/kg) caused notable therapeutic effects in the VaD mouse model, providing a promising lead or chemical probe for investigating the biological functions of PDE9 inhibition. Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Animals; Binding Sites; Catalytic Domain; Dementia, Vascular; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Half-Life; Humans; Maze Learning; Mice; Molecular Docking Simulation; Phosphodiesterase Inhibitors; Protein Isoforms; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship	2019

Article

Year

Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.

Journal of medicinal chemistry, 2019, 04-25, Volume: 62, Issue:8

To identify phosphodiesterase-9 (PDE9) as a novel target for the treatment of vascular dementia (VaD), a series of pyrazolopyrimidinone analogues were discovered based on a hit 1. Hit-to-lead optimization resulted in a potent inhibitor 2 with excellent selectivity and physicochemical properties to enable in vivo studies. Oral administration of 2 (5.0 mg/kg) caused notable therapeutic effects in the VaD mouse model, providing a promising lead or chemical probe for investigating the biological functions of PDE9 inhibition.

Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Animals; Binding Sites; Catalytic Domain; Dementia, Vascular; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Half-Life; Humans; Maze Learning; Mice; Molecular Docking Simulation; Phosphodiesterase Inhibitors; Protein Isoforms; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2019