The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
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 |
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 |
26562545 |
13 |
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 |
26430878 |
102 |
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 |
26288344 |
15 |
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 |
25592707 |
31 |
Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors. |
Washington University |
25801159 |
36 |
Discovery of novel pyrazolopyrimidinone analogs as potent inhibitors of phosphodiesterase type-5. |
Csir-Indian Institute of Integrative Medicine |
24785301 |
83 |
Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD. |
Astrazeneca |
9873708 |
16 |
N-arylrolipram derivatives as potent and selective PDE4 inhibitors. |
Novartis Horsham Research Center |
23421315 |
18 |
Novel inhibitors of protein arginine deiminase with potential activity in multiple sclerosis animal model. |
University Health Network |
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 |
22963052 |
38 |
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1. |
Vu University Amsterdam |
22891752 |
18 |
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 |
22889281 |
36 |
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate. |
Novartis Institutes For Biomedical Research |
21456625 |
41 |
Elucidation of a structural basis for the inhibitor-driven, p62 (SQSTM1)-dependent intracellular redistribution of cAMP phosphodiesterase-4A4 (PDE4A4). |
University of Glasgow |
18686943 |
28 |
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. |
Matrix Laboratories |
17228876 |
36 |
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 |
16168647 |
80 |
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 |
10691693 |
64 |
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 |
12270195 |
15 |
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 |
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 |
12031319 |
46 |
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor. |
Merck Frosst Centre For Therapeutic Research |
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 |
21983442 |
142 |
Synthesis and structure-activity relationship studies of dihydronaphthyridinediones as a novel structural class of potent and selective PDE7 inhibitors. |
Biocrea |
21871695 |
46 |
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 |
20933411 |
69 |
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 |
20825218 |
69 |
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors. |
RhôNe-Poulenc Rorer |
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 |
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 |
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 |
19339180 |
69 |
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents. |
Pfizer |
18945617 |
50 |
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 |
18835163 |
41 |
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 |
16516471 |
114 |
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors. |
Merck Frosst Center For Therapeutic Research |
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 |
12773045 |
27 |
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 |
12749899 |
17 |
Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors. |
Merck Frosst Centre For Therapeutic Research |
12639571 |
24 |
Substituted aminopyridines as potent and selective phosphodiesterase-4 inhibitors. |
Merck Frosst Centre For Therapeutic Research |
12031318 |
45 |
CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors. |
Celltech R&D |
11052785 |
14 |
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 |
26908025 |
164 |
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design. |
Vrije Universiteit Amsterdam |
10091677 |
15 |
Substituted furans as inhibitors of the PDE4 enzyme. |
Merck Frosst Centre For Therapeutic Research |
9873643 |
75 |
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors. |
Novartis Pharma |
30888810 |
48 |
Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors. |
Sun Yat-Sen University |
9464356 |
24 |
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 |
23585921 |
52 |
Synthesis and |
Washington University School of Medicine |
30052440 |
5 |
Lead-like Drugs: A Perspective. |
Pfizer |
30245400 |
167 |
Discovery of furyl/thienyl ?-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect. |
Shandong University |
29353721 |
63 |
Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis. |
Seoul National University |
29152042 |
32 |
Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases. |
Therachem Research Medilab (India) |
28698053 |
2 |
Stable C-N axial chirality in 1-aryluracil scaffold and differences in in vitro metabolic clearance between atropisomers of PDE4 inhibitor. |
Osaka University |
28613871 |
18 |
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 |
9349523 |
22 |
Cloning and expression of a human serotonin 5-HT4 receptor cDNA. |
Janssen Research Foundation |
9305929 |
19 |
Expression cloning of a rat hypothalamic galanin receptor coupled to phosphoinositide turnover. |
Synaptic Pharmaceutical |
9303569 |
35 |
Characterization of human serotonin 1D and 1B receptors using [3H]-GR-125743, a novel radiolabelled serotonin 5HT1D/1B receptor antagonist. |
RhôNe-Poulenc Rorer |
17643112 |
12 |
Splicing factor SF3b as a target of the antitumor natural product pladienolide. |
Eisai |
18790640 |
22 |
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 |
17629487 |
20 |
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists. |
Seoul National University |