176 articles for thisTarget
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The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.
Smithkline Beecham Pharmaceuticals
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.
Universidad De Navarra
Synthesis of a tritium-labeled indolidan analogue and its use as a radioligand for phosphodiesterase-inhibitor cardiotonic binding sites.
Eli Lilly
Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and evaluation of potential prodrugs of lixazinone (N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2- oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide, RS-82856).
Syntex Research
Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents.
TBA
2-(beta-Arylethylamino)- and 4-(beta-arylethylamino)quinazolines as phosphodiesterase inhibitors.
TBA
3D-QSAR studies on thieno[3,2-d]pyrimidines as phosphodiesterase IV inhibitors.
National Institute of Pharmaceutical Education and Research (NIPER)
Comparative molecular field analysis (CoMFA) of phthalazine derivatives as phosphodiesterase IV inhibitors.
National Institute of Pharmaceutical Education and Research
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.
Tanabe Seiyaku
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Celltech R&D
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Celltech R&D
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
Zambon Group
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
Zambon Group
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
Zambon Group
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
Celltech-Chiroscience
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.
Institut De Recherche Jouveinal-Parke Davis
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.
RhôNe-Poulenc Rorer
Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.
Rh£Ne-Poulenc Rorer Central Research
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.
Rh£Ne-Poulenc Rorer Central Research
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.
Chiroscience
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
Rh£Ne-Poulenc Rorer Central Research
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
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.
Intra-Cellular Therapies
Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors.
Sanofi Research Center
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
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
Southern Medical University
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 a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Bristol-Myers Squibb R & D
Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).
Novartis Institutes For Biomedical Research
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.
Washington University
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Merck Research Laboratories
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.
Csir-Indian Institute of Integrative Medicine
Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
Merck Serono
Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.
Astrazeneca
N-arylrolipram derivatives as potent and selective PDE4 inhibitors.
Novartis Horsham Research Center
Novel inhibitors of protein arginine deiminase with potential activity in multiple sclerosis animal model.
University Health Network
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
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Vu University Amsterdam
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.
Universidade Federal Do Rio De Janeiro
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Novartis Institutes For Biomedical Research
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4).
University of Glasgow
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
Matrix Laboratories
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Pfizer
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Merck Frosst Centre For Therapeutic Research
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
Monash University (Parkville Campus)
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
Tanabe Seiyaku
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
Novartis Pharma
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
Tanabe Seiyaku
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.
Smithkline Beecham Pharmaceuticals
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.
Tanabe Seiyaku
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Merck Frosst Centre For Therapeutic Research
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
Novartis Pharma
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Merck Frosst Centre For Therapeutic Research
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
Pfizer
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.
Biocrea
Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.
RhôNe-Poulenc Rorer
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.
Merck Frosst Centre For Therapeutic Research
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.
RhôNe-Poulenc Rorer
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.
Merck Frosst Centre For Therapeutic Research
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors.
Biotie Therapies
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Pfizer
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Pfizer
The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAggIII conditions
TBA
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.
Pfizer
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
Pfizer
Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: identification of MK-0873, a potent and effective PDE4 inhibitor.
Merck Frosst Center For Therapeutic Research
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
Merck Frosst Center For Therapeutic Research
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
Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review.
University of Louisiana At Lafayette
Peptidylarginine deiminases 4 as a promising target in drug discovery.
Zhejiang Ocean University
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.
Pfizer
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Merck
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.
Glaxosmithkline
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Merck Frosst Centre For Therapeutic Research
Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.
Merck Frosst Centre For Therapeutic Research
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors.
Merck Frosst Centre For Therapeutic Research
Advances in the Development of Phosphodiesterase-4 Inhibitors.
Sichuan Academy of Medical Science & Sichuan Provincial People'S Hospital
Discovery of sulfonyl hydrazone derivative as a new selective PDE4A and PDE4D inhibitor by lead-optimization approach on the prototype LASSBio-448: In vitro and in vivo preclinical studies.
Universidade Federal Do Rio De Janeiro
CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors.
Celltech R&D
Discovery of 2-((R)-4-(2-Fluoro-4-(methylsulfonyl)phenyl)-2-methylpiperazin-1-yl)-N-((1R,2s,3S,5S,7S)-5-hydroxyadamantan-2-yl)pyrimidine-4-carboxamide (SKI2852): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of 11?-Hydroxysteroid Dehydrogenase Type 1 (11?-HSD1).
Sk Chemicals
Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation.
Andhra University
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.
Changzhou University
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
Merck Frosst Centre For Therapeutic Research
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
Vrije Universiteit Amsterdam
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
1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.
Tanabe Seiyaku
Substituted furans as inhibitors of the PDE4 enzyme.
Merck Frosst Centre For Therapeutic Research
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
Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.
Bristol-Myers Squibb Research & Development
Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.
Pfizer
Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.
Hokuriku University
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
Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.
Dainippon Sumitomo Pharma
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.
Chiesi Farmaceutici
Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
Pfizer
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
Celgene
Functionalized pyrazoles and pyrazolo[3,4-d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity.
Universit£
Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.
Umr Cnrs 7081
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
Vrije Universiteit
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.
Vrije Universiteit
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
Vrije Universiteit
Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.
Wyeth Research
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
Vrije Universiteit
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
Vrije Universiteit
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
Pfizer
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Smithkline Beecham Pharmaceuticals
Synthesis of 7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and novel derivatives free of positional isomers. Potent inhibitors of cAMP-specific phosphodiesterase and of malignant tumor cell growth.
University of Kaiserslautern
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
Sw 8 Rh£Ne-Poulenc Rorer Central Research
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.
RhôNe-Poulenc Rorer
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
Pfizer
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.
Hokuriku University
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
Dipartimento Di Scienze Farmaceutiche, Firenze, Italy.
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
Pfizer
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Shandong University
Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.
Seoul National University
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
Centre De Neurochimie Du Cnrs
Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases.
Therachem Research Medilab (India)
Stable C-N axial chirality in 1-aryluracil scaffold and differences in in vitro metabolic clearance between atropisomers of PDE4 inhibitor.
Osaka University
Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38? MAPK/PDE-4 Inhibitor with Activity against TNF?-Related Diseases.
C-A-I-R Biosciences
Effects of alkyl substitutions of xanthine skeleton on bronchodilation.
Hokuriku University
The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor.
University of Frankfurt
Cloning and expression of a human serotonin 5-HT4 receptor cDNA.
Janssen Research Foundation
Expression cloning of a rat hypothalamic galanin receptor coupled to phosphoinositide turnover.
Synaptic Pharmaceutical
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist.
RhôNe-Poulenc Rorer
Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: chemistry, biological activities, and molecular modeling.
Abbott Laboratories
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Seoul National University