Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Small-molecule phosphodiesterase probes: discovery of potent and selective CNS-penetrable quinazoline inhibitors of PDE1

Journal Article · · MedChemComm
DOI:https://doi.org/10.1039/C4MD00113C· OSTI ID:1346245
Abstract not provided
Research Organization:
Advanced Photon Source (APS), Argonne National Laboratory (ANL), Argonne, IL (US)
Sponsoring Organization:
USDOE Office of Science (SC)
OSTI ID:
1346245
Journal Information:
MedChemComm, Journal Name: MedChemComm Journal Issue: 9 Vol. 5; ISSN 2040-2503
Publisher:
Royal Society of Chemistry
Country of Publication:
United States
Language:
ENGLISH

References (22)

Preclinical Characterization of Selective Phosphodiesterase 10A Inhibitors: A New Therapeutic Approach to the Treatment of Schizophrenia journal February 2008
Defining Desirable Central Nervous System Drug Space through the Alignment of Molecular Properties, in Vitro ADME, and Safety Attributes journal March 2010
PDE Inhibition and cognition enhancement journal April 2012
Phosphodiesterase genes are associated with susceptibility to major depression and antidepressant treatment response journal September 2006
Cyclic 3′,5′-nucleotide phosphodiesterase journal February 1970
Biochemistry and Physiology of Cyclic Nucleotide Phosphodiesterases: Essential Components in Cyclic Nucleotide Signaling journal June 2007
Cyclic nucleotide phosphodiesterase (PDE) superfamily: A new target for the development of specific therapeutic agents journal March 2006
Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1 H -pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia † Coordinates of the PDE10A crystal structures have been deposited in the Protein Data Bank for compound 1 (3HQW), 2 (3HQY), 3 (3HQW) and 9 (3HR1). journal August 2009
Unusual Tethering Effects in the Schmidt Reaction of Hydroxyalkyl Azides with Ketones:  Cation−π and Steric Stabilization of a Pseudoaxial Phenyl Group journal November 2003
Protective effects of phosphodiesterase-1 (PDE1) and ATP sensitive potassium (KATP) channel modulators against 3-nitropropionic acid induced behavioral and biochemical toxicities in experimental Huntington׳s disease journal June 2014
Discovery of a Series of 6,7-Dimethoxy-4-pyrrolidylquinazoline PDE10A Inhibitors journal January 2007
1-Indancarboxylic acids. I. Electrophilic substitution reactions of 1-indancarboxylic acid and synthesis of 6-substituted 1-indancarboxylic acids as potential antiinflammatory agents. journal January 1977
Calcium dependent phosphodiesterase activity and its activating factor (PAF) from brain journal December 1970
Inhibition of the striatum-enriched phosphodiesterase PDE10A: A novel approach to the treatment of psychosis journal August 2006
Potent Tetracyclic Guanine Inhibitors of PDE1 and PDE5 Cyclic Guanosine Monophosphate Phosphodiesterases with Oral Antihypertensive Activity journal July 1997
Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties journal March 2010
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-[[3,4-(methylenedioxy)benzyl]amino]-6,7,8-trimethoxyquinazoline journal November 1993
Phosphodiesterases in the CNS: targets for drug development journal August 2006
Molecular cloning and characterization of a calmodulin-dependent phosphodiesterase enriched in olfactory sensory neurons. journal October 1995
Catalytic Enantioselective Construction of All-Carbon Quaternary Stereocenters:  Synthetic and Mechanistic Studies of the C-Acylation of Silyl Ketene Acetals journal April 2005
Cyclic GMP Phosphodiesterase Inhibitors. 2. Requirement of 6-Substitution of Quinazoline Derivatives for Potent and Selective Inhibitory Activity journal June 1994
Cyclic nucleotide phosphodiesterases and their role in endocrine cell signaling journal January 2002

Similar Records

Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors
Journal Article · Fri Aug 09 00:00:00 EDT 2019 · Bioorg. Med. Chem. Lett. · OSTI ID:1557274

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1
Journal Article · Wed May 02 00:00:00 EDT 2018 · Journal of Medicinal Chemistry · OSTI ID:1499732

Discovery of Potent Small-Molecule Inhibitors of MLL Methyltransferase
Journal Article · Thu Jul 16 00:00:00 EDT 2020 · ACS Medicinal Chemistry Letters · OSTI ID:1642220

Related Subjects