Proteins > cAMP-specific 3',5'-cyclic phosphodiesterase 4B
Page last updated: 2024-08-07 17:02:22
cAMP-specific 3',5'-cyclic phosphodiesterase 4B
A 3,5-cyclic-AMP phosphodiesterase 4B that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q07343]
Synonyms
EC 3.1.4.53;
DPDE4;
PDE32
Research
Bioassay Publications (155)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 7 (4.52) | 18.7374 |
1990's | 28 (18.06) | 18.2507 |
2000's | 50 (32.26) | 29.6817 |
2010's | 57 (36.77) | 24.3611 |
2020's | 13 (8.39) | 2.80 |
Compounds (79)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
theophylline | Homo sapiens (human) | IC50 | 527.7500 | 4 | 4 |
theophylline | Homo sapiens (human) | Ki | 530.0000 | 1 | 1 |
denbufylline | Homo sapiens (human) | IC50 | 0.0851 | 2 | 2 |
dipyridamole | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
fluoxetine | Homo sapiens (human) | Ki | 1.5600 | 1 | 1 |
ibudilast | Homo sapiens (human) | IC50 | 1.7100 | 3 | 3 |
amrinone | Homo sapiens (human) | IC50 | 113.6000 | 4 | 5 |
1-methyl-3-isobutylxanthine | Homo sapiens (human) | IC50 | 23.5700 | 3 | 3 |
losartan | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
milrinone | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
pentoxifylline | Homo sapiens (human) | IC50 | 90.0000 | 1 | 1 |
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone | Homo sapiens (human) | IC50 | 18.9333 | 2 | 3 |
4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone | Homo sapiens (human) | Ki | 1.9300 | 1 | 1 |
rolipram | Homo sapiens (human) | IC50 | 17.0012 | 89 | 99 |
rolipram | Homo sapiens (human) | Ki | 1.2577 | 14 | 18 |
streptonigrin | Homo sapiens (human) | IC50 | 1.8700 | 1 | 1 |
thalidomide | Homo sapiens (human) | IC50 | 500.0000 | 1 | 1 |
trequinsin | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
zardaverine | Homo sapiens (human) | IC50 | 71.4748 | 5 | 14 |
1-hydroxyphthalazine | Homo sapiens (human) | IC50 | 0.5200 | 1 | 1 |
9-benzyladenine | Homo sapiens (human) | IC50 | 160.0000 | 1 | 1 |
8-bromo cyclic adenosine monophosphate | Homo sapiens (human) | IC50 | 18.4667 | 2 | 3 |
cartazolate | Homo sapiens (human) | IC50 | 0.1995 | 1 | 1 |
enoximone | Homo sapiens (human) | IC50 | 52.6333 | 3 | 3 |
imazodan | Homo sapiens (human) | IC50 | 6.0000 | 1 | 1 |
nitraquazone | Homo sapiens (human) | IC50 | 0.0500 | 1 | 1 |
cipamfylline | Homo sapiens (human) | IC50 | 1.9000 | 1 | 1 |
cipamfylline | Homo sapiens (human) | Ki | 21.0000 | 1 | 1 |
ethyl 3-amino-1h-pyrazole-4-carboxylate | Homo sapiens (human) | IC50 | 200.0000 | 1 | 2 |
8-((4-chlorophenyl)thio)cyclic-3',5'-amp | Homo sapiens (human) | IC50 | 81.3333 | 2 | 3 |
8-thio-benzyl cyclic amp | Homo sapiens (human) | IC50 | 29.0000 | 2 | 3 |
8-chloro-cyclic adenosine monophosphate | Homo sapiens (human) | IC50 | 34.3333 | 2 | 3 |
tadalafil | Homo sapiens (human) | IC50 | 66.9007 | 6 | 16 |
4-phenylpyrrolidone-2 | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 2 |
cdp 840 | Homo sapiens (human) | IC50 | 0.1028 | 6 | 7 |
7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine | Homo sapiens (human) | IC50 | 0.0160 | 1 | 1 |
9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
9-(2-hydroxy-3-nonyl)adenine | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
cilomilast | Homo sapiens (human) | IC50 | 14.3675 | 26 | 39 |
cilomilast | Homo sapiens (human) | Ki | 0.0380 | 2 | 2 |
rp 73401 | Homo sapiens (human) | IC50 | 11.4984 | 21 | 32 |
rp 73401 | Homo sapiens (human) | Ki | 0.0011 | 6 | 6 |
moracin c | Homo sapiens (human) | IC50 | 18.1000 | 1 | 1 |
(+)-rolipram | Homo sapiens (human) | IC50 | 1.3500 | 2 | 2 |
n(6)-benzyl-cyclic adenosine 5'-monophosphate | Homo sapiens (human) | IC50 | 68.0000 | 2 | 3 |
betulinan a | Homo sapiens (human) | IC50 | 44.0000 | 1 | 1 |
moracin m | Homo sapiens (human) | IC50 | 4.5000 | 1 | 1 |
mesembrenone | Homo sapiens (human) | IC50 | 0.4700 | 1 | 1 |
cocaine | Homo sapiens (human) | Ki | 1.1150 | 1 | 1 |
rolipram | Homo sapiens (human) | IC50 | 0.3666 | 11 | 11 |
mesopram | Homo sapiens (human) | IC50 | 0.4200 | 2 | 2 |
roflumilast | Homo sapiens (human) | IC50 | 31.8660 | 30 | 39 |
roflumilast | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
cyclic nucleotide phosphodiesterases, type 4 | Homo sapiens (human) | IC50 | 0.0290 | 2 | 3 |
hc 030031 | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
3-(n,n-dimethylsulfonamido)-4-methyl-nitrobenzene | Homo sapiens (human) | IC50 | 117.2667 | 3 | 3 |
4,5-dihydro-6-(4-(imidazol-1-yl)phenyl)-5-methyl-3(2h)-pyridazinone | Homo sapiens (human) | Ki | 50.0000 | 2 | 6 |
tetomilast | Homo sapiens (human) | IC50 | 0.0740 | 1 | 1 |
indolidan | Homo sapiens (human) | IC50 | 0.1500 | 1 | 1 |
fosbretabulin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
sch 351591 | Homo sapiens (human) | IC50 | 0.0600 | 3 | 3 |
rs 14203 | Homo sapiens (human) | IC50 | 0.0050 | 2 | 2 |
gsk 256066 | Homo sapiens (human) | IC50 | 0.0000 | 4 | 4 |
ci 1044 | Homo sapiens (human) | IC50 | 0.2700 | 1 | 1 |
l-454,560 | Homo sapiens (human) | IC50 | 0.0008 | 6 | 7 |
t 1032 | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
8-(methylthio)cyclic 3',5'-adenosine monophosphate | Homo sapiens (human) | IC50 | 39.0000 | 2 | 3 |
apremilast | Homo sapiens (human) | IC50 | 0.0590 | 7 | 7 |
f-amidine | Homo sapiens (human) | IC50 | 110.8000 | 2 | 2 |
8-benzylthio-n(6)-n-butyladenosine cyclic-3,5'-monophosphate | Homo sapiens (human) | IC50 | 40.0000 | 2 | 3 |
3-(2,5-dimethoxyphenyl)-6-(3,4-dimethoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine | Homo sapiens (human) | IC50 | 3.3618 | 3 | 3 |
n-alpha-benzoyl-n5-(2-chloro-1-iminoethyl)-l-ornithine amide | Homo sapiens (human) | IC50 | 5.9000 | 1 | 1 |
an2728 | Homo sapiens (human) | IC50 | 10.1796 | 7 | 7 |
bms-911543 | Homo sapiens (human) | IC50 | 5.6000 | 1 | 1 |
gsk1210151a | Homo sapiens (human) | IC50 | 3.9811 | 1 | 1 |
chf6001 | Homo sapiens (human) | IC50 | 0.0000 | 3 | 3 |
sildenafil | Homo sapiens (human) | IC50 | 23.5251 | 11 | 20 |
zaprinast | Homo sapiens (human) | IC50 | 24.3333 | 3 | 3 |
zaprinast | Homo sapiens (human) | Ki | 43.1267 | 2 | 6 |
vardenafil | Homo sapiens (human) | IC50 | 6.6668 | 3 | 12 |
Imidazosagatriazinone | Homo sapiens (human) | IC50 | 0.5000 | 1 | 1 |
pelrinone | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
lixazinone | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
rolipram | Homo sapiens (human) | EC50 | 0.6600 | 2 | 2 |
Drugs with Other Measurements
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
2-(beta-Arylethylamino)- and 4-(beta-arylethylamino)quinazolines as phosphodiesterase inhibitors.Journal of medicinal chemistry, , Volume: 28, Issue:1, 1985
Substituted 6,7-dihydroimidazo[1,2-a]purin-9(4H)-ones.Journal of medicinal chemistry, , Volume: 23, Issue:11, 1980
Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.Journal of medicinal chemistry, , May-23, Volume: 45, Issue:11, 2002
Novel and selective calcitonin-inducing agents.Journal of medicinal chemistry, , Mar-23, Volume: 43, Issue:6, 2000
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Phosphodiesterase inhibitors. Part 1: Synthesis and structure-activity relationships of pyrazolopyridine-pyridazinone PDE inhibitors developed from ibudilast.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 21, Issue:11, 2011
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.Journal of medicinal chemistry, , Volume: 34, Issue:10, 1991
Synthesis and cardiotonic activity of novel biimidazoles.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Novel quinoline-based derivatives: A new class of PDE4B inhibitors for adjuvant-induced arthritis.European journal of medicinal chemistry, , Aug-05, Volume: 238, 2022
PdClEuropean journal of medicinal chemistry, , Oct-05, Volume: 221, 2021
Novel cyanothiouracil and cyanothiocytosine derivatives as concentration-dependent selective inhibitors of U87MG glioblastomas: Adenosine receptor binding and potent PDE4 inhibition.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
New imidazopyridines with phosphodiesterase 4 and 7 inhibitory activity and their efficacy in animal models of inflammatory and autoimmune diseases.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Synthesis and SAR Studies of 1ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
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.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors.European journal of medicinal chemistry, , Dec-01, Volume: 207, 2020
Ultrasound assisted rapid synthesis of mefenamic acid based indole derivatives under ligand free Cu-catalysis: Their pharmacological evaluation.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 30, Issue:10, 2020
Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.Bioorganic & medicinal chemistry letters, , 11-15, Volume: 29, Issue:22, 2019
InClEuropean journal of medicinal chemistry, , Jul-15, Volume: 174, 2019
Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.European journal of medicinal chemistry, , Apr-15, Volume: 168, 2019
Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 28, Issue:19, 2018
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 28, Issue:7, 2018
Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.Bioorganic & medicinal chemistry letters, , 10-15, Volume: 28, Issue:19, 2018
Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]Bioorganic & medicinal chemistry, , 03-15, Volume: 25, Issue:6, 2017
Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry, , 10-15, Volume: 25, Issue:20, 2017
Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis and bioactivity of pyrazole and triazole derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 26, Issue:15, 2016
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Design, synthesis and biological evaluation of novel tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.Bioorganic & medicinal chemistry, , Nov-15, Volume: 23, Issue:22, 2015
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Novel Roflumilast analogs as soft PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Montmorillonite K-10 catalyzed green synthesis of 2,6-unsubstituted dihydropyridines as potential inhibitors of PDE4.European journal of medicinal chemistry, , Volume: 62, 2013
Benzoquinones and terphenyl compounds as phosphodiesterase-4B inhibitors from a fungus of the order Chaetothyriales (MSX 47445).Journal of natural products, , Mar-22, Volume: 76, Issue:3, 2013
Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
C-C bond formation at C-2 of a quinoline ring: synthesis of 2-(1H-indol-3-yl)quinoline-3-carbonitrile derivatives as a new class of PDE4 inhibitors.Bioorganic & medicinal chemistry, , Apr-01, Volume: 20, Issue:7, 2012
Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.Journal of medicinal chemistry, , Sep-13, Volume: 55, Issue:17, 2012
Identification of chalcones as potent and selective PDE5A1 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Dual inhibitors of phosphodiesterase-4 and serotonin reuptake.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Identification of a potent new chemotype for the selective inhibition of PDE4.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Rhodanine derivatives as novel inhibitors of PDE4.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 18, Issue:6, 2008
A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.Bioorganic & medicinal chemistry letters, , Volume: 16, Issue:3, 2006
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.Bioorganic & medicinal chemistry letters, , Feb-11, Volume: 12, Issue:3, 2002
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.Bioorganic & medicinal chemistry letters, , Jan-08, Volume: 11, Issue:1, 2001
Synthesis and biological evaluation of 2,5-dihydropyrazol.Bioorganic & medicinal chemistry letters, , Dec-04, Volume: 10, Issue:23, 2000
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.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.Bioorganic & medicinal chemistry letters, , Oct-02, Volume: 10, Issue:19, 2000
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.Bioorganic & medicinal chemistry letters, , Sep-18, Volume: 10, Issue:18, 2000
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.Journal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Orally active indole N-oxide PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 8, Issue:2, 1998
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.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
Aryl sulfonamides as selective PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Thalidomide analogs and PDE4 inhibition.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.Journal of medicinal chemistry, , May-09, Volume: 40, Issue:10, 1997
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Design and synthesis of conformationally constrained analogues of 4-(3-butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as potent inhibitors of cAMP-specific phosphodiesterase.Journal of medicinal chemistry, , Nov-24, Volume: 38, Issue:24, 1995
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-specifiJournal of medicinal chemistry, , Dec-22, Volume: 38, Issue:26, 1995
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.Journal of medicinal chemistry, , Apr-28, Volume: 38, Issue:9, 1995
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones.Journal of medicinal chemistry, , Dec-25, Volume: 35, Issue:26, 1992
Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.Journal of medicinal chemistry, , Volume: 32, Issue:7, 1989
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Design and synthesis of 4,5,6,7-tetrahydro-1H-1,2-diazepin-7-one derivatives as a new series of Phosphodiesterase 4 (PDE4) inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 27, Issue:1, 2017
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
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.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Synthesis and molecular modeling of novel tetrahydro-β-carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.Journal of medicinal chemistry, , Jan-27, Volume: 54, Issue:2, 2011
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
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.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.Bioorganic & medicinal chemistry letters, , Jan-20, Volume: 8, Issue:2, 1998
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
Zinc enzymes in medicinal chemistry.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
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.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Discovery of selective PDE4B inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 19, Issue:12, 2009
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.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Orally active PDE4 inhibitors with therapeutic potential.Bioorganic & medicinal chemistry letters, , Mar-08, Volume: 14, Issue:5, 2004
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
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.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.Bioorganic & medicinal chemistry letters, , Jan-08, Volume: 11, Issue:1, 2001
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
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.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Water-soluble PDE4 inhibitors for the treatment of dry eye.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
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.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-25, Volume: 12, Issue:4, 2002
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.Bioorganic & medicinal chemistry letters, , Jan-07, Volume: 12, Issue:1, 2002
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.Bioorganic & medicinal chemistry letters, , Jan-08, Volume: 11, Issue:1, 2001
The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.Bioorganic & medicinal chemistry letters, , Oct-02, Volume: 10, Issue:19, 2000
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Orally active indole N-oxide PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Nov-03, Volume: 8, Issue:21, 1998
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.Journal of medicinal chemistry, , Jun-18, Volume: 41, Issue:13, 1998
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.Journal of medicinal chemistry, , Jan-29, Volume: 41, Issue:3, 1998
2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 8, Issue:19, 1998
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.Journal of medicinal chemistry, , May-27, Volume: 37, Issue:11, 1994
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
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.Journal of medicinal chemistry, , Jan-25, Volume: 50, Issue:2, 2007
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Zinc enzymes in medicinal chemistry.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
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.European journal of medicinal chemistry, , Oct-15, Volume: 204, 2020
InClEuropean journal of medicinal chemistry, , Jul-15, Volume: 174, 2019
Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 28, Issue:7, 2018
[no title available]European journal of medicinal chemistry, , Mar-25, Volume: 148, 2018
4-Amino-7,8-dihydro-1,6-naphthyridin-5(6 H)-ones as Inhaled Phosphodiesterase Type 4 (PDE4) Inhibitors: Structural Biology and Structure-Activity Relationships.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.Journal of medicinal chemistry, , 10-13, Volume: 59, Issue:19, 2016
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.Journal of medicinal chemistry, , 12-08, Volume: 59, Issue:23, 2016
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 24, Issue:1, 2014
Novel Roflumilast analogs as soft PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 24, Issue:18, 2014
Phosphodiesterase inhibitors. Part 6: design, synthesis, and structure-activity relationships of PDE4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory activity.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 23, Issue:19, 2013
Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.Bioorganic & medicinal chemistry, , Nov-15, Volume: 21, Issue:22, 2013
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual β₂-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Identification of the fused bicyclic 4-amino-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.Bioorganic & medicinal chemistry letters, , May-01, Volume: 22, Issue:9, 2012
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.Bioorganic & medicinal chemistry, , Mar-15, Volume: 18, Issue:6, 2010
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 19, Issue:5, 2009
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.Journal of medicinal chemistry, , May-19, Volume: 48, Issue:10, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Novel amide derivatives of 1,3-dimethyl-2,6-dioxopurin-7-yl-alkylcarboxylic acids as multifunctional TRPA1 antagonists and PDE4/7 inhibitors: A new approach for the treatment of pain.European journal of medicinal chemistry, , Oct-05, Volume: 158, 2018
Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 17, Issue:18, 2007
Synthesis and profile of SCH351591, a novel PDE4 inhibitor.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Zinc enzymes in medicinal chemistry.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
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.Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 20, Issue:18, 2010
Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 15, Issue:23, 2005
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
InClEuropean journal of medicinal chemistry, , Jul-15, Volume: 174, 2019
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
4-Amino-7,8-dihydro-1,6-naphthyridin-5(6 H)-ones as Inhaled Phosphodiesterase Type 4 (PDE4) Inhibitors: Structural Biology and Structure-Activity Relationships.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors.Bioorganic & medicinal chemistry, , 11-15, Volume: 24, Issue:22, 2016
Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.Journal of medicinal chemistry, , Mar-26, Volume: 52, Issue:6, 2009
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 19, Issue:13, 2009
Identification of a potent new chemotype for the selective inhibition of PDE4.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 18, Issue:4, 2008
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.European journal of medicinal chemistry, , Mar-05, Volume: 213, 2021
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Lead-like Drugs: A Perspective.Journal of medicinal chemistry, , 12-13, Volume: 61, Issue:23, 2018
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Advances in the Development of Phosphodiesterase-4 Inhibitors.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
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.Journal of medicinal chemistry, , 05-23, Volume: 62, Issue:10, 2019
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.Journal of medicinal chemistry, , Aug-11, Volume: 59, Issue:15, 2016
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Identification of chalcones as potent and selective PDE5A1 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
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.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
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.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 13, Issue:14, 2003
Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.Bioorganic & medicinal chemistry letters, , Mar-25, Volume: 12, Issue:6, 2002
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
Identification of chalcones as potent and selective PDE5A1 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine: highly potent and selective PDE4 inhibitors.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
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.Journal of medicinal chemistry, , Oct-09, Volume: 46, Issue:21, 2003
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.Journal of medicinal chemistry, , Feb-18, Volume: 37, Issue:4, 1994
Synthesis of quinoline derivatives: discovery of a potent and selective phosphodiesterase 5 inhibitor for the treatment of Alzheimer's disease.European journal of medicinal chemistry, , Volume: 60, 2013
Optimization of purine based PDE1/PDE5 inhibitors to a potent and selective PDE5 inhibitor for the treatment of male ED.Bioorganic & medicinal chemistry letters, , May-02, Volume: 15, Issue:9, 2005
Structural basis for the activity of drugs that inhibit phosphodiesterases.Structure (London, England : 1993), , Volume: 12, Issue:12, 2004
Enables
This protein enables 8 target(s):
Target | Category | Definition |
3',5'-cyclic-AMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic AMP + H2O = AMP + H+. [GOC:ai, RHEA:25277] |
calcium channel regulator activity | molecular function | Modulates the activity of a calcium channel. [GOC:mah] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
cAMP binding | molecular function | Binding to cAMP, the nucleotide cyclic AMP (adenosine 3',5'-cyclophosphate). [GOC:ai] |
gamma-tubulin binding | molecular function | Binding to the microtubule constituent protein gamma-tubulin. [GOC:jl] |
transmembrane transporter binding | molecular function | Binding to a transmembrane transporter, a protein or protein complex that enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:BHF, GOC:jl, PMID:33199372] |
metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
3',5'-cyclic-GMP phosphodiesterase activity | molecular function | Catalysis of the reaction: 3',5'-cyclic GMP + H2O = GMP + H+. [RHEA:16957] |
Located In
This protein is located in 7 target(s):
Target | Category | Definition |
centrosome | cellular component | A structure comprised of a core structure (in most organisms, a pair of centrioles) and peripheral material from which a microtubule-based structure, such as a spindle apparatus, is organized. Centrosomes occur close to the nucleus during interphase in many eukaryotic cells, though in animal cells it changes continually during the cell-division cycle. [GOC:mah, ISBN:0198547684] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
synaptic vesicle | cellular component | A secretory organelle, typically 50 nm in diameter, of presynaptic nerve terminals; accumulates in high concentrations of neurotransmitters and secretes these into the synaptic cleft by fusion with the 'active zone' of the presynaptic plasma membrane. [PMID:10099709, PMID:12563290] |
postsynaptic density | cellular component | An electron dense network of proteins within and adjacent to the postsynaptic membrane of an asymmetric, neuron-neuron synapse. Its major components include neurotransmitter receptors and the proteins that spatially and functionally organize them such as anchoring and scaffolding molecules, signaling enzymes and cytoskeletal components. [GOC:BHF, GOC:dos, GOC:ef, GOC:jid, GOC:pr, GOC:sjp, http://molneuro.kaist.ac.kr/psd, PMID:14532281, Wikipedia:Postsynaptic_density] |
Z disc | cellular component | Platelike region of a muscle sarcomere to which the plus ends of actin filaments are attached. [GOC:mtg_muscle, ISBN:0815316194] |
dendritic spine | cellular component | A small, membranous protrusion from a dendrite that forms a postsynaptic compartment, typically receiving input from a single presynapse. They function as partially isolated biochemical and an electrical compartments. Spine morphology is variable:they can be thin, stubby, mushroom, or branched, with a continuum of intermediate morphologies. They typically terminate in a bulb shape, linked to the dendritic shaft by a restriction. Spine remodeling is though to be involved in synaptic plasticity. [GOC:nln] |
excitatory synapse | cellular component | A synapse in which an action potential in the presynaptic cell increases the probability of an action potential occurring in the postsynaptic cell. [GOC:dph, GOC:ef] |
Active In
This protein is active in 3 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
perinuclear region of cytoplasm | cellular component | Cytoplasm situated near, or occurring around, the nucleus. [GOC:jid] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Part Of
This protein is part of 2 target(s):
Target | Category | Definition |
gamma-tubulin complex | cellular component | A multiprotein complex composed of gamma-tubulin and other non-tubulin proteins. Gamma-tubulin complexes are localized to microtubule organizing centers, and play an important role in the nucleation of microtubules. The number and complexity of non-tubulin proteins associated with these complexes varies between species. [GOC:clt, PMID:12134075] |
voltage-gated calcium channel complex | cellular component | A protein complex that forms a transmembrane channel through which calcium ions may pass in response to changes in membrane potential. [GOC:mah] |
Involved In
This protein is involved in 15 target(s):
Target | Category | Definition |
neutrophil homeostasis | biological process | The process of regulating the proliferation and elimination of neutrophils such that the total number of neutrophils within a whole or part of an organism is stable over time in the absence of an outside stimulus. [GOC:add, GOC:pr, PMID:12752675, PMID:12960266] |
cAMP catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of the nucleotide cAMP (cyclic AMP, adenosine 3',5'-cyclophosphate). [ISBN:0198506732] |
neutrophil chemotaxis | biological process | The directed movement of a neutrophil cell, the most numerous polymorphonuclear leukocyte found in the blood, in response to an external stimulus, usually an infection or wounding. [GOC:jl, ISBN:0198506732] |
positive regulation of type II interferon production | biological process | Any process that activates or increases the frequency, rate, or extent of interferon-gamma production. Interferon-gamma is also known as type II interferon. [GOC:add, GOC:mah, PMID:15546383] |
positive regulation of interleukin-2 production | biological process | Any process that activates or increases the frequency, rate, or extent of interleukin-2 production. [GOC:mah] |
T cell receptor signaling pathway | biological process | The series of molecular signals initiated by the cross-linking of an antigen receptor on a T cell. [GOC:add] |
leukocyte migration | biological process | The movement of a leukocyte within or between different tissues and organs of the body. [GOC:add, ISBN:0781735149, PMID:14680625, PMID:14708592, PMID:7507411, PMID:8600538] |
cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
cellular response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organism exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:krc, GOC:mah] |
cellular response to epinephrine stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an epinephrine stimulus. Epinephrine is a catecholamine that has the formula C9H13NO3; it is secreted by the adrenal medulla to act as a hormone, and released by certain neurons to act as a neurotransmitter active in the central nervous system. [GOC:BHF, GOC:mah] |
negative regulation of adenylate cyclase-activating adrenergic receptor signaling pathway | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of an adenylate cyclase-activating adrenergic receptor protein signaling pathway activity. An adrenergic receptor signaling pathway is the series of molecular signals generated as a consequence of an adrenergic receptor binding to one of its physiological ligands. [GOC:BHF, GOC:mah] |
regulation of cardiac muscle cell contraction | biological process | Any process that modulates the frequency, rate or extent of cardiac muscle cell contraction. [GOC:BHF, GOC:mtg_cardiac_conduct_nov11] |
negative regulation of relaxation of cardiac muscle | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of relaxation of cardiac muscle. [GOC:BHF, GOC:rl, GOC:TermGenie, PMID:19708671] |
regulation of calcium ion transmembrane transport via high voltage-gated calcium channel | biological process | Any process that modulates the frequency, rate or extent of generation of calcium ion transmembrane transport via high voltage-gated calcium channel. [GOC:dph, GOC:pg, GOC:TermGenie, PMID:1611048] |
cAMP-mediated signaling | biological process | An intracellular signaling cassette that starts with production of cyclic AMP (cAMP), and ends with activation of downstream effectors that further transmit the signal within the cell. [GOC:signaling] |