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 |
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 |
26976215 |
5 |
Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action. |
Vanderbilt University School Of Medicine |
26935942 |
41 |
Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. |
Mercachem |
26681511 |
33 |
Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors. |
Sanofi Research Center |
26526739 |
35 |
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships. |
Southern Medical University |
26288683 |
43 |
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms. |
Bristol-Myers Squibb R & D |
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 |
25936260 |
8 |
Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors. |
University Of Genoa |
26005524 |
147 |
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. |
Merck Research Laboratories |
25815146 |
29 |
Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors. |
Janssen Pharmaceutica |
25736998 |
37 |
Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors. |
Merck Serono |
25126889 |
10 |
Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors. |
University Of Genoa |
24998378 |
62 |
Discovery of triazines as selective PDE4B versus PDE4D inhibitors. |
Northern Illinois University |
24984230 |
22 |
Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis. |
Leo Pharma |
25075977 |
12 |
Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi. |
Sun Yat-Sen University |
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 |
25264825 |
54 |
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors. |
Centro De Investigaciones Biol�Gicas (Csic) |
25221665 |
33 |
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement. |
Janssen Pharmaceutica |
25149511 |
34 |
Novel Roflumilast analogs as soft PDE4 inhibitors. |
Amakem |
24785301 |
83 |
Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD. |
Astrazeneca |
24597921 |
14 |
Prenylated coumarins: natural phosphodiesterase-4 inhibitors from Toddalia asiatica. |
Sun Yat-Sen University |
9873708 |
16 |
N-arylrolipram derivatives as potent and selective PDE4 inhibitors. |
Novartis Horsham Research Center |
23294698 |
8 |
Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors. |
University Of Hyderabad Campus |
23149228 |
60 |
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux. |
Amgen |
22985069 |
18 |
Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design. |
Sun Yat-Sen University |
22963052 |
38 |
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1. |
Vu University Amsterdam |
22944118 |
27 |
Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model. |
Glenmark Pharmaceuticals |
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 |
22385507 |
20 |
Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds. |
Instituto De Qu£Mica M£Dica (Csic) |
22483586 |
10 |
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor. |
Sun Yat-Sen University |
22401864 |
61 |
Discovery of oxazole-based PDE4 inhibitors with picomolar potency. |
Merck Research Laboratories |
20188577 |
23 |
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas. |
King'S College London |
19014888 |
52 |
Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. |
Human Biomolecular Research Institute |
18686943 |
28 |
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease. |
Matrix Laboratories |
17337182 |
23 |
Potent and selective xanthine-based inhibitors of phosphodiesterase 5. |
Novartis Institutes Of Biomedical Research |
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 |
15887951 |
29 |
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases. |
Monash University (Parkville Campus) |
11405657 |
123 |
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives. |
Tanabe Seiyaku |
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 |
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 |
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 |
22030030 |
5 |
Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2. |
Monash University (Parkville Campus) |
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 |
19447034 |
76 |
Discovery of selective PDE4B inhibitors. |
Asahi Kasei Pharma |
21602043 |
50 |
Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors. |
H. Lundbeck |
21087867 |
30 |
Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors. |
Universit£ |
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 |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical And Public Health Institute |
20709547 |
69 |
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors. |
Merck Frosst Centre For Therapeutic Research |
20202838 |
62 |
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors. |
Pfizer |
19361990 |
7 |
Surface plasmon resonance-based detection of ladder-shaped polyethers by inhibition detection method. |
Osaka University |
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 |
19744860 |
19 |
Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors. |
Kyoto 601-8550 |
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 |
19827751 |
21 |
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms. |
University Of Genoa |
19339180 |
69 |
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents. |
Pfizer |
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 |
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 |
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 |
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 |
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 |
10197972 |
133 |
1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor. |
Tanabe Seiyaku |
9873643 |
75 |
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors. |
Novartis Pharma |
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 |
10087018 |
11 |
Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity. |
University Of Rochester |
9349523 |
22 |
Cloning and expression of a human serotonin 5-HT4 receptor cDNA. |
Janssen Research Foundation |
7684450 |
26 |
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 |