The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28686445 |
39 |
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 |
28406621 |
65 |
Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties. |
Dart Neuroscience |
28165743 |
37 |
Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders. |
Dart Neuroscience |
27597413 |
58 |
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 |
27606546 |
218 |
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 |
27301679 |
21 |
Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket. |
Takeda Pharmaceutical |
26978121 |
20 |
Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4. |
Sun Yat-Sen University |
26789933 |
100 |
Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases. |
Intra-Cellular Therapies |
26935942 |
41 |
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. |
Mercachem |
26526739 |
35 |
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships. |
Southern Medical University |
25866242 |
55 |
2-(Isopropylamino)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as selective phosphodiesterase 7 inhibitors with potent in vivo efficacy. |
Kaken Pharmaceutical |
25801159 |
36 |
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5. |
Csir-Indian Institute of Integrative Medicine |
25754491 |
11 |
8-(3-chloro-4-methoxybenzyl)-8H-pyrido[2,3-d]pyrimidin-7-one derivatives as potent and selective phosphodiesterase 5 inhibitors. |
Mitsubishi Tanabe Pharma |
25529739 |
43 |
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 |
25456383 |
113 |
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility. |
TBA |
25455484 |
26 |
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 |
25442307 |
17 |
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 |
25432025 |
34 |
Discovery of a phosphodiesterase 9A inhibitor as a potential hypoglycemic agent. |
Sun Yat-Sen University |
24856068 |
48 |
Pharmacophore based virtual screening, molecular docking and biological evaluation to identify novel PDE5 inhibitors with vasodilatory activity. |
Banasthali University |
24758746 |
36 |
Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia. |
Janssen Pharmaceutica |
24702184 |
5 |
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors. |
Chinese Academy of Sciences (Cas) |
23313637 |
14 |
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease. |
Columbia University |
23260348 |
91 |
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 |
18045743 |
49 |
Bioactivities of a series of phosphodiesterase type 5 (PDE-5) inhibitors as modelled by MIA-QSAR. |
Universidade Federal De Lavras-Ufla |
18656371 |
47 |
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil. |
Universidade Federal De Lavras-Ufla |
17553682 |
33 |
3D-QSAR studies on sildenafil analogues, selective phosphodiesterase 5 inhibitors. |
Sungkyunkwan University |
23137303 |
38 |
Design, synthesis, and pharmacological evaluation of monocyclic pyrimidinones as novel inhibitors of PDE5. |
Chinese Academy of Sciences |
22985069 |
18 |
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design. |
Sun Yat-Sen University |
22780914 |
35 |
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 |
22607677 |
8 |
Identification of chalcones as potent and selective PDE5A1 inhibitors. |
Youai |
22204607 |
15 |
Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds. |
University of Lille |
22483586 |
10 |
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor. |
Sun Yat-Sen University |
22377514 |
75 |
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia. |
Merck Research Laboratories |
20400309 |
26 |
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. |
Pfizer |
20443228 |
35 |
1-(2-Ethoxyethyl)-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors. |
Pfizer |
18778098 |
12 |
Potent inhibition of human phosphodiesterase-5 by icariin derivatives. |
University of Milan |
17337182 |
23 |
Potent and selective xanthine-based inhibitors of phosphodiesterase 5. |
Novartis Institutes of Biomedical Research |
15771456 |
21 |
Pyrroloquinolone PDE5 inhibitors with improved pharmaceutical profiles for clinical studies on erectile dysfunction. |
Johnson & Johnson Pharmaceutical Research and Development |
15887951 |
29 |
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. |
Monash University (Parkville Campus) |
15878277 |
42 |
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives. |
Chinese Academy of Sciences |
14521414 |
44 |
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 |
12213052 |
15 |
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction. |
Johnson & Johnson Pharmaceutical Research & Development |
11405657 |
123 |
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives. |
Tanabe Seiyaku |
10891111 |
56 |
4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. |
Eisai |
10090791 |
77 |
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. |
Tanabe Seiyaku |
9191951 |
8 |
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors. |
Upr 421 Du Cnrs |
8709099 |
20 |
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 |
8568820 |
10 |
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 |
7658441 |
89 |
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities. |
Biofor |
8254606 |
55 |
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline. |
Eisai |
8388468 |
37 |
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase. |
Smithkline Beecham Pharmaceuticals |
12824030 |
67 |
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors. |
Tanabe Seiyaku |
11755362 |
24 |
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 |
12161123 |
13 |
A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. |
Korea Institute of Science & Technology |
22222034 |
35 |
The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia. |
Merck Research Laboratories |
22142545 |
96 |
Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia. |
Merck Research Laboratories |
22100260 |
30 |
The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. |
Pfizer |
21988093 |
316 |
Highly potent, selective, and orally active phosphodiesterase 10A inhibitors. |
Pfizer |
21955943 |
47 |
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region. |
Pfizer |
21920746 |
1 |
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam. |
University of Strasburg |
21983442 |
142 |
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors. |
Biocrea |
19447034 |
76 |
Discovery of selective PDE4B inhibitors. |
Asahi Kasei Pharma |
21602043 |
50 |
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors. |
H. Lundbeck |
21570840 |
44 |
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1. |
Merck Research Laboratories |
21530250 |
73 |
Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast. |
Heriot-Watt University |
21189023 |
66 |
Synthesis and molecular modeling of novel tetrahydro-ß-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties. |
German University In Cairo |
21087867 |
30 |
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors. |
Universit£ |
20937560 |
54 |
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 |
20709547 |
69 |
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
Merck Frosst Centre For Therapeutic Research |
20450197 |
80 |
Discovery of imidazo[1,5-a]pyrido[3,2-e]pyrazines as a new class of phosphodiesterase 10A inhibitiors. |
Biotie Therapies |
20206015 |
22 |
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 |
19856955 |
2 |
Lorneic acids, trialkyl-substituted aromatic acids from a marine-derived actinomycete. |
Nippon Suisan Kaisha |
20053559 |
55 |
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 |
20196613 |
32 |
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 |
19906530 |
22 |
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 |
19631533 |
126 |
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 |
19919087 |
55 |
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy. |
Pfizer |
19540112 |
33 |
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors. |
Pfizer |
19539468 |
6 |
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system. |
Pfizer |
| 5 |
The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAggIII conditions |
TBA |
| 71 |
Imidazotriazinone inhibitors of the Ca2+-calmodulin sensitive phosphodiesterase (PDE I) |
TBA |
| 36 |
Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction |
TBA |
19339180 |
69 |
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents. |
Pfizer |
19272774 |
12 |
Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
19049349 |
107 |
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 |
18976905 |
35 |
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction. |
Chong Kun Dang Research Institute |
18951784 |
19 |
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule. |
Pfizer |
18393409 |
16 |
Synthesis and pharmacological evaluations of sildenafil analogues for treatment of erectile dysfunction. |
State University of Campinas |
17107795 |
13 |
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil. |
Inserm U761 Biostructures and Drug Discovery Lille |
16913726 |
33 |
Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction. |
Università |
16337379 |
14 |
Identification of phosphodiesterase-1 and 5 dual inhibitors by a ligand-based virtual screening optimized for lead evolution. |
Sumitomo Pharmaceuticals |
16275071 |
26 |
A new chemical tool for exploring the physiological function of the PDE2 isozyme. |
Pfizer |
16263279 |
37 |
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function. |
Pfizer |
16005625 |
162 |
Discovery of hydroxamic acid analogs as dual inhibitors of phosphodiesterase-1 and -5. |
Sumitomo Pharmaceuticals |
15993055 |
61 |
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors. |
Bayer Healthcare |
15837329 |
37 |
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors. |
RhôNe-Poulenc Rorer |
15837326 |
51 |
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED. |
Schering-Plough Research Institute |
15324877 |
90 |
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives. |
Pfizer |
15324876 |
94 |
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1. |
Pfizer |
15324874 |
169 |
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies. |
Pfizer |
15149695 |
24 |
New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors. |
Pfizer |
15125967 |
30 |
Identification of purine inhibitors of phosphodiesterase 7 (PDE7). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15080987 |
20 |
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 |
15006407 |
15 |
Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
14980684 |
52 |
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction. |
Schering-Plough Research Institute |
14736245 |
16 |
Structure-activity relationships of N-acyl pyrroloquinolone PDE-5 inhibitors. |
Johnson and Johnson Pharmaceutical Research and Development |
14521415 |
44 |
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 |
12668004 |
76 |
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors. |
Pfizer |
12639576 |
37 |
Synthesis and biological activities of novel beta-carbolines as PDE5 inhibitors. |
Johnson & Johnson Pharmaceutical Research & Development |
12570368 |
9 |
Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12540243 |
29 |
Furoyl and benzofuroyl pyrroloquinolones as potent and selective PDE5 inhibitors for treatment of erectile dysfunction. |
Johnson & Johnson Pharmaceutical Research & Development |
12372521 |
21 |
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors. |
Schering-Plough Research Institute |
12182866 |
83 |
8-Aryl xanthines potent inhibitors of phosphodiesterase 5. |
Novartis Horsham Research Centre |
11958981 |
25 |
Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors. |
Bayer |
11606139 |
11 |
Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents. |
Institute of Pharmaceutical Chemistry |
11549447 |
6 |
The discovery of novel, potent and selective PDE5 inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
32171616 |
32 |
Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease. |
Changzhou University |
11297448 |
11 |
Substituted pyrazolopyridines as potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
32603117 |
32 |
Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis. |
Sun Yat-Sen University |
11150175 |
17 |
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
27491708 |
31 |
Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors. |
Janssen Research & Development |
26908025 |
164 |
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design. |
Vrije Universiteit Amsterdam |
10753463 |
5 |
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
32115956 |
46 |
Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia. |
Guangzhou University of Chinese Medicine |
31158744 |
53 |
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model. |
Universit£ |
31099559 |
36 |
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 |
31021628 |
50 |
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 |
30916555 |
43 |
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia. |
Sun Yat-Sen University |
10197972 |
133 |
1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor. |
Tanabe Seiyaku |
9990447 |
51 |
Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors. |
Schering-Plough Research Institute |
30554955 |
34 |
Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects. |
Changzhou University |
30509781 |
22 |
Design, synthesis and evaluation of N |
Kasetsart University |
9873594 |
44 |
Aryl sulfonamides as selective PDE4 inhibitors. |
Chiroscience |
30888810 |
48 |
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
Sun Yat-Sen University |
31103902 |
41 |
Multi-target design strategies for the improved treatment of Alzheimer's disease. |
China Pharmaceutical University |
31235264 |
13 |
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 |
30986068 |
112 |
Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability. |
TBA |
9719589 |
13 |
4-Benzylamino-1-chloro-6-substituted phthalazines: synthesis and inhibitory activity toward phosphodiesterase 5. |
Eisai |
9435906 |
26 |
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors. |
Schering-Plough Research Institute |
9216839 |
113 |
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity. |
Schering-Plough Research Institute |
31610942 |
65 |
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 |
8648603 |
101 |
Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones. |
Laboratories Glaxo Wellcome Centre De Recherches |
8544172 |
3 |
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 |
25062128 |
16 |
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 |
24400806 |
101 |
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases. |
Chiesi Farmaceutici |
8201604 |
96 |
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. |
RhôNe-Poulenc Rorer |
8120866 |
54 |
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. |
Smithkline Beecham Pharmaceuticals |
8027992 |
49 |
Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity. |
Eisai |
23867165 |
21 |
Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5. |
Chinese Academy of Sciences |
6620311 |
9 |
Optical resolution, absolute configuration, and activity of the enantiomers of proxyphylline. |
TBA |
30245400 |
167 |
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect. |
Shandong University |
30148362 |
36 |
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 |
29549837 |
151 |
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 |
29505934 |
31 |
Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors. |
Shandong University |
29620890 |
25 |
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations. |
Glaxosmithkline |
29363967 |
11 |
Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease. |
Sun Yat-Sen University |
29545101 |
55 |
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors. |
South China Agricultural University |
2544722 |
94 |
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues. |
Centre De Neurochimie Du Cnrs |
29291443 |
30 |
Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study. |
Sun Yat-Sen University |
29456790 |
5 |
Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189. |
Pfizer |
29718668 |
27 |
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1. |
Pfizer |
28751142 |
27 |
Design, synthesis and biological evaluation of dual acetylcholinesterase and phosphodiesterase 5A inhibitors in treatment for Alzheimer's disease. |
Central South University |
28796496 |
67 |
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 |
28759228 |
36 |
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders. |
Takeda Pharmaceutical |
29293004 |
12 |
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. |
Pfizer |
29200281 |
20 |
Discovery and Optimization of Thiazolidinyl and Pyrrolidinyl Derivatives as Inhaled PDE4 Inhibitors for Respiratory Diseases. |
Chiesi Farmaceutici |
28985058 |
20 |
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 |
| 8 |
Synthesis,MolecularModeling, and Biological Evaluation of Novel Tetrahydro-ß-Carboline Hydantoin and Tetrahydro-ß-Carboline Thiohydantoin Derivatives as Phosphodiesterase 5 Inhibitors |
German University In Cairo |
22356915 |
27 |
Biological and structural characterization of Trypanosoma cruzi phosphodiesterase C and Implications for design of parasite selective inhibitors. |
University of North Carolina |
22284362 |
91 |
Identification of biologically active PDE11-selective inhibitors using a yeast-based high-throughput screen. |
Boston College |
16759100 |
33 |
A novel series of potent and selective PDE5 inhibitors with potential for high and dose-independent oral bioavailability. |
Pfizer |