A new chemical tool for exploring the physiological function of the PDE2 isozyme

• Published in: Bioorganic & medicinal chemistry letters Vol. 16; no. 2; pp. 307 - 310
• Main Authors: Chambers, Robert J., Abrams, Kristin, Garceau, Norman Y., Kamath, Ajith V., Manley, Christopher M., Lilley, Susan C., Otte, Douglas A., Scott, Dennis O., Sheils, Alissa L., Tess, David A., Vellekoop, A. Samuel, Zhang, Yan, Lam, Kelvin T.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 15-01-2006; Elsevier
• Subjects: Adenine - analogs & derivatives; Adenine - pharmacology; Administration, Oral; Analytical, structural and metabolic biochemistry; Animals; Biological and medical sciences; Cyclic Nucleotide Phosphodiesterases, Type 2; Drug Evaluation, Preclinical; Enzymes and enzyme inhibitors; Fundamental and applied biological sciences. Psychology; Hydrolases; Indoles - chemical synthesis; Indoles - chemistry; Indoles - pharmacokinetics; Isoenzymes - drug effects; Isoenzymes - physiology; Medical sciences; Miscellaneous; Molecular Structure; PDE2; Pharmacology. Drug treatments; Phosphodiesterase; Phosphodiesterase Inhibitors - chemical synthesis; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - pharmacokinetics; Phosphoric Diester Hydrolases - drug effects; Phosphoric Diester Hydrolases - physiology; Rats; Solubility; Structure-Activity Relationship; PDE2; Phosphodiesterase; Rat; 3',5'-Cyclic-GMP phosphodiesterase; Isozyme; Lactam; Esterases; Selectivity; Phosphoric diester hydrolases; Thiadiazole derivatives; Aromatic compound; Oxygen nitrogen heterocycle; Sulfur nitrogen heterocycle; Absorption Distribution Metabolisme Excretion; Enzyme; Rodentia; Oral administration; Enzyme inhibitor; Bioavailability; Tricyclic compound; In vitro; In vivo; Vertebrata; Mammalia; Animal; Hydrolases; Pharmacokinetics
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2005.10.005

Oxindole (
2) is a potent and selective PDE2 inhibitor with a favorable ADME, physiochemical and pharmacokinetic profile to allow for use as a chemical tool in elucidating the physiological role of PDE2.
Oxindole (
2) is a potent and selective PDE2 inhibitor with a favorable ADME, physiochemical and pharmacokinetic profile to allow for use as a chemical tool in elucidating the physiological role of PDE2.