214 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
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
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, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
University of Navarra
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
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.
Southern Medical University
2-(Isopropylamino)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as selective phosphodiesterase 7 inhibitors with potent in vivo efficacy.
Kaken Pharmaceutical
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5.
Csir-Indian Institute of Integrative Medicine
8-(3-chloro-4-methoxybenzyl)-8H-pyrido[2,3-d]pyrimidin-7-one derivatives as potent and selective phosphodiesterase 5 inhibitors.
Mitsubishi Tanabe Pharma
Discovery and SAR study of 2-(4-pyridylamino)thieno[3,2-d]pyrimidin-4(3H)-ones as soluble and highly potent PDE7 inhibitors.
Kyoto 607-8042
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
TBA
The discovery of avanafil for the treatment of erectile dysfunction: a novel pyrimidine-5-carboxamide derivative as a potent and highly selective phosphodiesterase 5 inhibitor.
Mitsubishi Tanabe Pharma
Design and synthesis of novel 5-(3,4,5-trimethoxybenzoyl)-4-aminopyrimidine derivatives as potent and selective phosphodiesterase 5 inhibitors: scaffold hopping using a pseudo-ring by intramolecular hydrogen bond formation.
Mitsubishi Tanabe Pharma
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent.
Sun Yat-Sen University
Pharmacophore based virtual screening, molecular docking and biological evaluation to identify novel PDE5 inhibitors with vasodilatory activity.
Banasthali University
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.
Janssen Pharmaceutica
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors.
Chinese Academy of Sciences (Cas)
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.
Columbia University
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
Bioactivities of a series of phosphodiesterase type 5 (PDE-5) inhibitors as modelled by MIA-QSAR.
Universidade Federal De Lavras-Ufla
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
Universidade Federal De Lavras-Ufla
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors.
Sungkyunkwan University
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5.
Chinese Academy of Sciences
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.
Sun Yat-Sen University
Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
Pfizer
Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.
University of Lille
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.
Sun Yat-Sen University
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Merck Research Laboratories
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Pfizer
1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Pfizer
Potent inhibition of human phosphodiesterase-5 by icariin derivatives.
University of Milan
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.
Novartis Institutes of Biomedical Research
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction.
Johnson & Johnson Pharmaceutical Research and Development
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
Monash University (Parkville Campus)
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
Chinese Academy of Sciences
The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1: 5,6,11,11a-tetrahydro-1H-imidazo[1',5':1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues.
Glaxosmithkline
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
Johnson & Johnson Pharmaceutical Research & Development
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
Tanabe Seiyaku
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Eisai
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
Tanabe Seiyaku
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
Tan£Be Seiyaku
Studies of cardiotonic agents. 8. Synthesis and biological activities of optically active 6-(4-(benzylamino)-7-quinazolinyl)-4,5-dihydro-5-methyl-3(2H)- pyridazinone (KF15232).
Kyowa Hakka
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities.
Biofor
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.
Eisai
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
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
A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5.
Korea Institute of Science & Technology
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
The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics.
Pfizer
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
Pfizer
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
University of Strasburg
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors.
Biocrea
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.
H. Lundbeck
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.
Merck Research Laboratories
Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast.
Heriot-Watt University
Synthesis and molecular modeling of novel tetrahydro-ß-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
German University In Cairo
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.
Universit£
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Dipartimento Di Scienze Farmaceutiche
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
Synthesis, molecular modeling and biological evaluation of novel tadalafil analogues as phosphodiesterase 5 and colon tumor cell growth inhibitors, new stereochemical perspective.
German University In Cairo
Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete.
Nippon Suisan Kaisha
Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors.
Korea Research Institute of Chemical Technology
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
Discovery of potent, selective, and orally bioavailable PDE5 inhibitor: Methyl-4-(3-chloro-4-methoxybenzylamino)-8-(2-hydroxyethyl)-7-methoxyquinazolin-6-ylmethylcarbamate (CKD 533).
Chong Kun Dang Research Institute
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
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
Pfizer
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Pfizer
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Pfizer
The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAggIII conditions
TBA
Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction
TBA
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.
Pfizer
Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.
Bristol-Myers Squibb Pharmaceutical Research Institute
Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.
Georgia State University
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
Chong Kun Dang Research Institute
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
Pfizer
Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction.
State University of Campinas
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Inserm U761 Biostructures and Drug Discovery Lille
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.
Università
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Menoufia University
Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.
Sun Yat-Sen University
Discovery and Structural Optimization of Toddacoumalone Derivatives as Novel PDE4 Inhibitors for the Topical Treatment of Psoriasis.
National-Local Joint Engineering Laboratory of Druggability and New Drugs Evaluation
Computational design, synthesis and biological evaluation of PDE5 inhibitors based on N
King Mongkut'S Institute of Technology
Pyrazole-containing pharmaceuticals: target, pharmacological activity, and their SAR studies.
Tianjin University
Identification of phosphodiesterase-1 and 5 dual inhibitors by a ligand-based virtual screening optimized for lead evolution.
Sumitomo Pharmaceuticals
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
Discovery of novel 2,3-dihydro-1H-inden-1-ones as dual PDE4/AChE inhibitors with more potency against neuroinflammation for the treatment of Alzheimer's disease.
Southern Medical University
Histone deacetylase 6 inhibitors with blood-brain barrier penetration as a potential strategy for CNS-Disorders therapy.
Shanghai Institute of Pharmaceutical Industry
Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5.
Sumitomo Pharmaceuticals
Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases: Discovery of ACT-672125.
Idorsia Pharmaceuticals
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.
Bayer Healthcare
Occurrence, synthesis and biological activity of 2-(2-phenyethyl)chromones.
Guizhou Medical University
Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.
Indian Institute of Technology (B.H.U.)
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
RhôNe-Poulenc Rorer
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.
Schering-Plough Research Institute
Paradigm shift of "classical" HDAC inhibitors to "hybrid" HDAC inhibitors in therapeutic interventions.
National Institute of Pharmaceutical Education and Research (NIPER)
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Pfizer
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Pfizer
Discovery of Potent Phosphodiesterase-9 Inhibitors for the Treatment of Hepatic Fibrosis.
Sun Yat-Sen University
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.
Pfizer
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Bristol-Myers Squibb Pharmaceutical Research Institute
Synthesis and phosphodiesterase 5 inhibitory activity of new sildenafil analogues containing a phosphonate group in the 5(')-sulfonamide moiety of phenyl ring.
Ewha Womans University
Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Merck
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.
Hainan University
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
Schering-Plough Research Institute
Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors.
Johnson and Johnson Pharmaceutical Research and Development
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment.
Chinese Academy of Sciences
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
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.
China Pharmaceutical University
From Celecoxib to a Novel Class of Phosphodiesterase 5 Inhibitors: Trisubstituted Pyrazolines as Novel Phosphodiesterase 5 Inhibitors with Extremely High Potency and Phosphodiesterase Isozyme Selectivity.
German University In Cairo
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
Pfizer
New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.
Palack£
Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors.
Johnson & Johnson Pharmaceutical Research & Development
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket.
Sun Yat-Sen University
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
Johnson & Johnson Pharmaceutical Research & Development
Design and synthesis of pyrazolo[3,4-d]pyrimidinone derivatives: Discovery of selective phosphodiesterase-5 inhibitors.
Cairo University
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.
Schering-Plough Research Institute
8-Aryl xanthines potent inhibitors of phosphodiesterase 5.
Novartis Horsham Research Centre
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.
Pfizer
Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents.
Institute of Pharmaceutical Chemistry
The discovery of novel, potent and selective PDE5 inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.
Changzhou University
Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.
Sun Yat-Sen University
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.
Bristol-Myers Squibb Pharmaceutical 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
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University of Chinese Medicine
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model.
Universit£
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
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.
Sun Yat-Sen University
1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.
Tanabe Seiyaku
Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.
Schering-Plough Research Institute
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
Multi-target design strategies for the improved treatment of Alzheimer's disease.
China Pharmaceutical 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
4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Eisai
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.
Schering-Plough Research Institute
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.
Schering-Plough Research Institute
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
Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones.
Laboratories Glaxo Wellcome Centre De Recherches
Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase.
Glaxo Wellcome Research
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
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.
Chiesi Farmaceutici
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
RhôNe-Poulenc Rorer
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Smithkline Beecham Pharmaceuticals
Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
Eisai
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.
Chinese Academy of Sciences
Optical resolution, absolute configuration, and activity of the enantiomers of proxyphylline.
TBA
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
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Shandong University
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
Design, synthesis, biological evaluation and in vivo testing of dual phosphodiesterase 5 (PDE5) and histone deacetylase 6 (HDAC6)-selective inhibitors for the treatment of Alzheimer's disease.
University of Navarra
Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors.
Shandong University
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.
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
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.
Centre De Neurochimie Du Cnrs
Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.
Sun Yat-Sen University
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.
Pfizer
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.
Pfizer
Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease.
Central South University
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
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Pfizer
Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases.
Chiesi Farmaceutici
Identification of a Novel 1,2,3,4-Tetrahydrobenzo[b][1,6]naphthyridine Analogue as a Potent Phosphodiesterase 5 Inhibitor with Improved Aqueous Solubility for the Treatment of Alzheimer's Disease.
Columbia University
Design, synthesis, and preliminary bioactivity evaluation of N(1) -hydroxyterephthalamide derivatives with indole cap as novel histone deacetylase inhibitors.
Shandong University