159 articles for thisTarget
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Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.
Dart Neuroscience
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.
Dart Neuroscience
Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.
Southern Medical University
Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket.
Takeda Pharmaceutical
Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.
Sun Yat-Sen University
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
Intra-Cellular Therapies
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.
Mercachem
Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.
Institute Of Radiopharmaceutical Cancer Research
Design, Synthesis, and Pharmacological Evaluation of 5,6-Disubstituted Pyridin-2(1H)-one Derivatives as Phosphodiesterase 10A (PDE10A) Antagonists.
Glenmark Research Centre
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
Southern Medical University
Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.
Takeda Pharmaceutical
Synthesis of Fluorine-Containing Phosphodiesterase 10A (PDE10A) Inhibitors and the In Vivo Evaluation of F-18 Labeled PDE10A PET Tracers in Rodent and Nonhuman Primate.
Washington University
Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.
Merck Research Laboratories
Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.
Merck Research Laboratories
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
Washington University
BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.
University Of Copenhagen
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.
Csir-Indian Institute Of Integrative Medicine
Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.
Universit£
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.
Glenmark Pharmaceuticals
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
TBA
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.
Sun Yat-Sen University
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
Amgen
Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.
Yamanouchi Pharmaceutical
Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.
Glenmark Pharmaceuticals
Radiosyntheses and in vivo evaluation of carbon-11 PET tracers for PDE10A in the brain of rodent and nonhuman primate.
Washington University
Development of a plate-based optical biosensor fragment screening methodology to identify phosphodiesterase 10A inhibitors.
Astrazeneca
PDE10 Inhibitors as Potential Treatment for Schizophrenia.
Therachem Research Medilab (India)
Discovery of a new series of [1,2,4]triazolo[4,3-a]quinoxalines as dual phosphodiesterase 2/phosphodiesterase 10 (PDE2/PDE10) inhibitors.
Janssen-Cilag
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.
Amgen
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Chinese Academy Of Sciences
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687).
Astrazeneca
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.
Sun Yat-Sen University
Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.
Amgen
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors.
St. John'S University
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
Monash University (Parkville Campus)
Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.
Amgen
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.
Astrazeneca
Pyrazoloquinolines as PDE10A inhibitors: discovery of a tool compound.
Merck Research Laboratories
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.
Merck Research Laboratories
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.
Merck Research Laboratories
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.
Biocrea
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
Washington University
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
H. Lundbeck
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.
Universit£
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.
Biotie Therapies
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
Pfizer
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Schering-Plough Research Institute
A new chemical tool for exploring the physiological function of the PDE2 isozyme.
Pfizer
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.
Pfizer
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Schering-Plough Research Institute
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.
Janssen Research & Development
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Vrije Universiteit Amsterdam
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Absolute Binding Free Energy Calculation and Design of a Subnanomolar Inhibitor of Phosphodiesterase-10.
Sun Yat-Sen University
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University Of Chinese Medicine
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Shanghai Institute Of Materia Medica
Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.
Chinese Academy Of Sciences
Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors.
Astellas Pharma
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.
Sun Yat-Sen University
Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.
Abbvie Deutschland
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
Changzhou University
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.
Sun Yat-Sen University
Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety.
Mitsubishi Tanabe Pharma
Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability.
TBA
Benzothiophene derivatives as phosphodiesterase 10A (PDE10A) inhibitors: Hit-to-lead studies.
Asubio Pharma
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.
South China Agricultural University
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors.
Astrazeneca
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Amgen
Discovery of benzo[d]imidazo[5,1-b]thiazole as a new class of phosphodiesterase 10A inhibitors.
Glenmark Pharmaceuticals
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Amgen
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.
H. Lundbeck
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Shandong University
Potential of PDE10A Inhibitors as Treatment for Schizophrenia and Other Neurological Disorders.
Therachem Research Medilab
Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.
Sun Yat-Sen University
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.
South China Agricultural University
Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.
Celon Pharma
Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.
Sun Yat-Sen University
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.
Pfizer
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Takeda Pharmaceutical
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
Takeda Pharmaceutical
Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.
Chiesi Farmaceutici
Design and optimization of purine derivatives as in vivo active PDE10A inhibitors.
Nanchang University
Inhibitory properties of ibuprofen and its amide analogues towards the hydrolysis and cyclooxygenation of the endocannabinoid anandamide.
Umeå University
Carbonic anhydrase inhibitors: inhibition of human and bovine isoenzymes by benzenesulphonamides, cyclitols and phenolic compounds.
Ondokuz Mayis University
Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.
Bristol-Myers Squibb
Lactosamine-Based Derivatives as Tools to Delineate the Biological Functions of Galectins: Application to Skin Tissue Repair.
Universit?? De Nantes
The chlorite dismutase (HemQ) from Staphylococcus aureus has a redox-sensitive heme and is associated with the small colony variant phenotype.
University Of Notre Dame
Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.
The University Of Calgary
Switching between allosteric and dimerization inhibition of HIV-1 protease.
Purdue University
Potent, exceptionally selective, orally bioavailable inhibitors of TNF-alpha Converting Enzyme (TACE): novel 2-substituted-1H-benzo[d]imidazol-1-yl)methyl)benzamide P1' substituents.
Bristol-Myers Squibb
Exploring inhibitor binding at the s' subsites of cathepsin L.
National Research Council Canada
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Bristol-Myers Squibb
Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate.
Morphochem
Structural and thermodynamic studies of simple aldose reductase-inhibitor complexes.
Medical College Of Wiscosin
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus.
Merck Research Laboratories
Synthesis and protein kinase C inhibitory activities of acyclic balanol analogs that are highly selective for protein kinase C over protein kinase A.
Sphinx Laboratories
2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity.
Parke-Davis Pharmaceutical Research
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
Dupont Pharmaceuticals
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a
Upjohn