Compounds > cilomilast
Page last updated: 2024-09-04

cilomilast and rolipram

cilomilast has been researched along with rolipram in 50 studies

Compound Research Comparison

Studies
(cilomilast)		Trials
(cilomilast)		Recent Studies (post-2010)
(cilomilast)		Studies
(rolipram)		Trials
(rolipram)		Recent Studies (post-2010) (rolipram)
16213421,60417401
162134226015

Protein Interaction Comparison

ProteinTaxonomycilomilast (IC50)rolipram (IC50)
cGMP-dependent 3',5'-cyclic phosphodiesteraseHomo sapiens (human)1.2233
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8AHomo sapiens (human)1.2233
Retina-specific copper amine oxidaseHomo sapiens (human)0.0003
cGMP-specific 3',5'-cyclic phosphodiesteraseHomo sapiens (human)1.0975
3',5'-cyclic-AMP phosphodiesterase Sus scrofa (pig)3.63
ReninHomo sapiens (human)3.5
Tumor necrosis factorHomo sapiens (human)0.35
cAMP-specific 3',5'-cyclic phosphodiesterase 4D Rattus norvegicus (Norway rat)0.7287
cAMP-specific 3',5'-cyclic phosphodiesterase 4CRattus norvegicus (Norway rat)0.7287
cAMP-specific 3',5'-cyclic phosphodiesterase 4BRattus norvegicus (Norway rat)0.8447
cAMP-specific 3',5'-cyclic phosphodiesterase 4AHomo sapiens (human)1.1942
Sodium-dependent serotonin transporterRattus norvegicus (Norway rat)0.095
Delta-type opioid receptorMus musculus (house mouse)1.5
Delta-type opioid receptorRattus norvegicus (Norway rat)1.5
cAMP-specific 3',5'-cyclic phosphodiesterase 4ARattus norvegicus (Norway rat)0.7287
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)0.835
cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)1.1005
cAMP-specific 3',5'-cyclic phosphodiesterase 4CHomo sapiens (human)1.61
cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)1.0794
cGMP-inhibited 3',5'-cyclic phosphodiesterase BHomo sapiens (human)0.835
cGMP-inhibited 3',5'-cyclic phosphodiesterase AHomo sapiens (human)2
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11AHomo sapiens (human)0.835
cAMP-specific 3',5'-cyclic phosphodiesterase 7BHomo sapiens (human)0.835
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10AHomo sapiens (human)0.835
Chain A, cAMP-specific phosphodiesterase PDE4D2Homo sapiens (human)0.33
Chain A, cAMP-specific phosphodiesterase PDE4D2Homo sapiens (human)0.33
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4BHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Chain A, cAMP-specific 3',5'-cyclic phosphodiesterase 4DHomo sapiens (human)0.288
Beta-2 adrenergic receptorCavia porcellus (domestic guinea pig)0.5

Research

Studies (50)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's5 (10.00)18.2507
2000's33 (66.00)29.6817
2010's10 (20.00)24.3611
2020's2 (4.00)2.80

Authors

AuthorsStudies
Andresen, CJ; Cheng, JB; Cohan, VL; Decker, C; DiCapua, FM; Duplantier, AJ; Johnson, KL; Kraus, KG; Turner, CR; UmLand, JP; Watson, JW; Wester, RT; Williams, AS; Williams, JA1
Bray-French, K; Hersperger, R; Mazzoni, L; Müller, T1
Auclair, E; Avenel, N; Bertin, B; Bigot, C; Burnouf, C; Calvet, A; Chan, K; Doherty, AM; Durand, C; Fasquelle, V; Féru, F; Gilbertsen, R; Jacobelli, H; Kebsi, A; Lallier, E; Maignel, J; Martin, B; Milano, S; Ouagued, M; Pascal, Y; Pruniaux, MP; Puaud, J; Rocher, MN; Terrasse, C; Wrigglesworth, R1
Ferlenga, P; Marchini, F; Morazzoni, G; Napoletano, M; Norcini, G; Pellacini, F; Pradella, L1
Kim, E; Kim, JH; Kim, SH; Nam, G; Rhee, CK; Shin, JH; Yoon, CM1
Fattori, R; Ferlenga, P; Marchini, F; Morazzoni, G; Napoletano, M; Norcini, G; Pellacini, F; Pradella, L1
Alonso, JM; Andrés, JI; Boeckx, G; Cools, M; de Chaffoy, D; De Clerck, F; Deroose, F; Díaz, A; Diels, G; Fernández, J; Freyne, EJ; Iturrino, L; Martínez, P; Matesanz, E; Megens, A; Peeters, D; Petit, D; Somers, M; Stoppie, P; Van Wauwe, J1
Boss, H; Couwenberg, D; Goubitz, K; Hatzelmann, A; Schenk, H; Sterk, GJ; Timmerman, H; Van der Mey, M1
Artis, DR; Bollag, G; Card, GL; England, BP; Fong, D; Gillette, S; Ibrahim, PN; Kim, SH; Lee, B; Luu, C; Milburn, MV; Powell, B; Schlessinger, J; Suzuki, Y; Tabrizizad, M; Zhang, KY1
Hughes, RA; Manallack, DT; Thompson, PE1
Bachert, EL; Cheng, JB; Cohan, VL; Duplantier, AJ; Jenkinson, TH; Kraus, KG; McKechney, MW; Pillar, JD; Watson, JW1
Bhirud, SB; Bhise, UN; Mashelkar, UC; Siva Kumar, BV; Vaidya, SD; Vinodkumar, R1
Jabaris, SS; Kodimuthali, A; Pal, M1
Barlow, DJ; Ehrman, TM; Hylands, PJ1
Barreiro, EJ; Bourguignon, JJ; Cardozo, SV; Fraga, CA; Justiniano, H; Kümmerle, AE; Lopes, AB; Lugnier, C; Martins, MA; Romeiro, NC; Schmitt, M; Villa, P1
Egerland, U; Gewald, R; Grunwald, C1
de Esch, IJ; de Graaf, C; Jansen, C; Kanev, GK; Kooistra, AJ; Leurs, R1
Bielska, M; Bruno, O; Bull, JA; Fossa, P; Giordanetto, F; Guariento, S; Iwanowa, X; Karawajczyk, A; Marchini, G1
Chen, W; Dong, G; Feng, C; Gu, Z; Li, H; Li, J; Li, M; Liu, H; Tang, W; Xu, Y; Zhang, R; Zhang, X; Zhu, F1
Balliano, TL; Barbosa, G; Carvalho, VF; da Silva, BA; de Souza, ET; Lima, LM; Martins, IRR; Martins, MA; Medeiros, MM; Moraes Junior, MO; Nunes, IKDC; Silva, PMR; Silva, SWD1
Barnette, MS; Christensen, SB; Essayan, DM; Grous, M; Kagey-Sobotka, A; Prabhakar, U; Rush, JA; Torphy, TJ1
Barnette, MS; Bartus, JO; Bender, PE; Bochnowicz, S; Burman, M; Christensen, SB; Cieslinski, LB; DeWolf, WE; Eggleston, DS; Forster, CJ; Gleason, JG; Griswold, DE; Grous, M; Guider, A; Haltiwanger, RC; Hillegas, LM; Karpinski, JM; Manning, CD; Osborn, RR; Ryan, MD; Torphy, TJ; Underwood, DC1
Au, BT; Collins, PD; Teixeira, MM; Williams, TJ1
Badger, AM; Barnette, MA; Christensen, S; Gorycki, PD; Griswold, DE; Grous, M; Levandoski, PA; Torphy, TJ; Webb, EF1
Chapman, R; Fine, J; Jones, H; Kreutner, W; Kung, TT; Minnicozzi, M; Spond, J1
Ezeamuzie, CI1
Cassali, GD; Poole, S; Souza, DG; Teixeira, MM1
Bornfeldt, KE; Lin, G1
Funk, RH; Kasper, M; Kuss, H; Plötze, K; Roth-Eichhorn, S; Schade, I; Schüler, S1
Devillier, P1
Barnette, MS; Cabrol, D; Ferré, F; Leroy, MJ; Méhats, C; Oger, S1
Astier, A; Bertrand, C; Jacob, C; Lagente, V; Martin-Chouly, CA; Pruniaux, MP1
Vignola, AM1
Allen, JM; Bertrand, C; Jacob, C; Lagente, V; Szilagyi, C1
Belleguic, C; Bertrand, C; Brinchault, G; Depincé, A; Lagente, V; Leportier-Comoy, C; Martin-Chouly, CA; Ouagued, M; Pruniaux, MP1
Darby-King, A; Harley, CW; McLean, JH1
Beume, R; Bundschuh, DS; Marx, D; Wohlsen, A; Wollin, L1
Advenier, C; Devillier, P; Fagon, JY; Faisy, C; Guerot, E; Naline, E; Risse, PA1
Baillie, GS; Camargo, LM; Castle, JC; Cheung, YF; Gall, I; Garrett-Engele, P; Houslay, MD; Johnson, JM; Kan, Z; Murdoch, H1
Chaves, J; Lerner, A; Makkinje, A; Meyers, JA; Taverna, J1
Harada, D; Ikeda, Y; Kobayashi, K; Manabe, H; Nosaka, Y1
Balachandran, S; Chaudhary, S; Dastidar, SG; Gupta, N; Nanda, K; Palle, V; Rajagopal, D; Ray, A; Seth, MK; Sharma, P; Shirumalla, R1
Ball, D; Barnette, MS; Capper-Spudich, EA; Davis, TG; Ferrari, L; Knowles, RG; Kou, JP; Lucas, FS; Nials, AT; Peterson, JJ; Podolin, PL; Solanke, YE; Williamson, RA; Wiseman, J; Wren, P1
Bertin, B; Bertrand, CP; Bouget, A; Burnouf, C; Doherty, AM; Dubuit, JP; Julien-Larose, C; Lagente, V; Leportier, C; Martin, B; Moreau, F; Ouaged, M; Pruniaux, MP; Rocher, MN1
Krug, O; Schänzer, W; Thevis, M1
Aguiar, JA; Ask, K; Cao, Q; Doxey, AC; Hirota, JA; Hou, V; Huff, RD; Inman, MD; Kim, Y; Miller, MS; Revill, S; Tiessen, N1
Hatzelmann, A; Sterk, GJ; Thibaut, U; Timmerman, H; Ulrich, WR; Van der Laan, IJ; Van der Mey, M; Van Klink, GP1
Boss, H; Hatzelmann, A; Sterk, GJ; Timmerman, H; Van der Laan, IJ; Van der Mey, M1
Huang, L; Jiang, HL; Lai, KF; Li, XS; Luo, ZH; Shan, WJ; Zhou, Q1
Huang, L; Lai, K; Li, X; Shan, W; Xie, J; Zhou, Q1

Reviews

4 review(s) available for cilomilast and rolipram

ArticleYear
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
    Journal of medicinal chemistry, 2005, May-19, Volume: 48, Issue:10

    Topics: Animals; Binding Sites; Crystallography, X-Ray; Cyclic AMP; Cyclic GMP; Drug Design; Humans; Models, Molecular; Molecular Structure; Phosphodiesterase Inhibitors; Quantitative Structure-Activity Relationship; Xanthines

2005
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
    Journal of medicinal chemistry, 2008, Sep-25, Volume: 51, Issue:18

    Topics: Asthma; Humans; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Pulmonary Disease, Chronic Obstructive

2008
[Physiopathology of COPD: choosing the right therapeutic targets].
    Revue de pneumologie clinique, 2003, Volume: 59, Issue:2 Pt 2

    Topics: Adrenal Cortex Hormones; Aged; Albuterol; Animals; Bacterial Infections; Bronchodilator Agents; Carboxylic Acids; Cyclohexanecarboxylic Acids; Disease Models, Animal; Drug Therapy, Combination; Humans; Inflammation; Mucociliary Clearance; Nitriles; Phosphodiesterase Inhibitors; Pulmonary Alveoli; Pulmonary Disease, Chronic Obstructive; Pulmonary Emphysema; Randomized Controlled Trials as Topic; Rats; Rolipram; Salmeterol Xinafoate; Smoking; Theophylline; Time Factors

2003
PDE4 inhibitors in COPD--a more selective approach to treatment.
    Respiratory medicine, 2004, Volume: 98, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Benzamides; Bronchodilator Agents; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Nitriles; Phosphodiesterase Inhibitors; Pneumonia; Pulmonary Disease, Chronic Obstructive; Rolipram; Theophylline; Treatment Outcome

2004

Trials

1 trial(s) available for cilomilast and rolipram

ArticleYear
The novel phosphodiesterase 4 inhibitor, CI-1044, inhibits LPS-induced TNF-alpha production in whole blood from COPD patients.
    Pulmonary pharmacology & therapeutics, 2005, Volume: 18, Issue:1

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adult; Azepines; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Dexamethasone; Dose-Response Relationship, Drug; Female; France; Humans; Male; Middle Aged; Niacinamide; Nitriles; Phosphodiesterase Inhibitors; Polysaccharides, Bacterial; Pulmonary Disease, Chronic Obstructive; Rolipram; Tumor Necrosis Factor-alpha

2005

Other Studies

45 other study(ies) available for cilomilast and rolipram

ArticleYear
7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
    Journal of medicinal chemistry, 1998, Jun-18, Volume: 41, Issue:13

    Topics: Airway Obstruction; Animals; Anti-Asthmatic Agents; Anti-Inflammatory Agents, Non-Steroidal; Bronchoalveolar Lavage Fluid; Cell Count; Cell Line; Cyclic AMP; Cytokines; Dihydropyridines; Drug Evaluation, Preclinical; Eosinophils; Guinea Pigs; Humans; In Vitro Techniques; Isoenzymes; Macaca fascicularis; Molecular Conformation; Neutrophils; Ovalbumin; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Pyrazoles; Pyrrolidinones; Rolipram; Structure-Activity Relationship

1998
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.
    Journal of medicinal chemistry, 2000, Feb-24, Volume: 43, Issue:4

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Animals; Anti-Asthmatic Agents; Asthma; Benzoates; Bronchoalveolar Lavage Fluid; Catalysis; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Enzyme Inhibitors; Eosinophils; Humans; In Vitro Techniques; Male; Naphthyridines; Palladium; Rats; Respiratory Burst; Structure-Activity Relationship

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, 2000, Dec-14, Volume: 43, Issue:25

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; 3',5'-Cyclic-GMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Anti-Inflammatory Agents, Non-Steroidal; Aorta; Azepines; Binding, Competitive; Brain; Bronchoalveolar Lavage; Cell Line; Cyclic Nucleotide Phosphodiesterases, Type 1; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclic Nucleotide Phosphodiesterases, Type 5; Dogs; Eosinophils; Ferrets; Guinea Pigs; Humans; In Vitro Techniques; Indoles; Isoenzymes; Male; Monocytes; Niacinamide; Ovalbumin; Phosphodiesterase I; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Radioligand Assay; Rats; Rats, Wistar; Structure-Activity Relationship; Trachea; Tumor Necrosis Factor-alpha; Vomiting

2000
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
    Bioorganic & medicinal chemistry letters, 2001, Jan-08, Volume: 11, Issue:1

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Benzamides; Biological Availability; Cyclic Nucleotide Phosphodiesterases, Type 4; Enzyme Inhibitors; Guinea Pigs; Humans; Inhibitory Concentration 50; Molecular Structure; Monocytes; Neutrophils; Phthalazines; Protein Binding; Pyridines; Rolipram; Tumor Necrosis Factor-alpha

2001
Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2001, Mar-12, Volume: 11, Issue:5

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Biological Assay; Cyclic Nucleotide Phosphodiesterases, Type 4; Humans; Molecular Structure; Phosphodiesterase Inhibitors; Pyrimidines; Quinazolines; Rats; Rolipram

2001
Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
    Bioorganic & medicinal chemistry letters, 2002, Jan-07, Volume: 12, Issue:1

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Binding Sites; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Drug Evaluation, Preclinical; Humans; Hydrogen Bonding; Neutrophils; Phosphodiesterase Inhibitors; Phthalazines; Rolipram; Structure-Activity Relationship

2002
Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2002, Feb-25, Volume: 12, Issue:4

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Topical; Animals; Anti-Inflammatory Agents; Cyclic Nucleotide Phosphodiesterases, Type 4; Disease Models, Animal; Dose-Response Relationship, Drug; Ear Diseases; Enzyme Inhibitors; Humans; Imidazoles; Inflammation; Inhibitory Concentration 50; Rats; Structure-Activity Relationship

2002
Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.
    Journal of medicinal chemistry, 2002, Jun-06, Volume: 45, Issue:12

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adamantane; Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzoates; Crystallography, X-Ray; Cyclic Nucleotide Phosphodiesterases, Type 4; Edema; Enzyme Inhibitors; Female; Humans; In Vitro Techniques; Mice; Molecular Conformation; Neutrophils; Phthalazines; Stereoisomerism; Structure-Activity Relationship

2002
Structural basis for the activity of drugs that inhibit phosphodiesterases.
    Structure (London, England : 1993), 2004, Volume: 12, Issue:12

    Topics: Binding Sites; Crystallography, X-Ray; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Protein Structure, Tertiary

2004
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, 2007, Jan-25, Volume: 50, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Biological Availability; Cyclic Nucleotide Phosphodiesterases, Type 4; Dogs; Eosinophils; Female; Ferrets; Heterocyclic Compounds, 3-Ring; Humans; In Vitro Techniques; Isoenzymes; Male; Phosphodiesterase Inhibitors; Pyrazoles; Pyridines; Rats; Recombinant Proteins; Structure-Activity Relationship; Triazoles; Vomiting

2007
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
    European journal of medicinal chemistry, 2008, Volume: 43, Issue:5

    Topics: Alkynes; Anti-Asthmatic Agents; Anti-Bacterial Agents; Benzimidazoles; Dipeptidyl-Peptidase IV Inhibitors; Heterocyclic Compounds, 2-Ring; Humans; Hypoglycemic Agents; Phosphodiesterase 4 Inhibitors; Protein Tyrosine Phosphatase, Non-Receptor Type 1; Structure-Activity Relationship

2008
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
    Bioorganic & medicinal chemistry, 2010, Mar-15, Volume: 18, Issue:6

    Topics: Anti-Inflammatory Agents; Crystallography, X-Ray; Cyclooxygenase 1; Cyclooxygenase 2; Databases, Factual; Drug Design; Drugs, Chinese Herbal; Enzyme Inhibitors; JNK Mitogen-Activated Protein Kinases; Medicine, Chinese Traditional; Models, Chemical; Models, Molecular; Molecular Conformation; p38 Mitogen-Activated Protein Kinases; Phosphodiesterase 4 Inhibitors; Structure-Activity Relationship

2010
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, 2012, Sep-13, Volume: 55, Issue:17

    Topics: Administration, Oral; Animals; Drug Design; Female; Humans; Hydrazones; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Models, Molecular; Molecular Conformation; Phosphodiesterase 4 Inhibitors; Pneumonia

2012
Discovery of triazines as potent, selective and orally active PDE4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Administration, Oral; Animals; Binding Sites; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclic Nucleotide Phosphodiesterases, Type 7; Drug Evaluation, Preclinical; Half-Life; Microsomes, Liver; Molecular Docking Simulation; Phosphodiesterase 4 Inhibitors; Protein Structure, Tertiary; Rats; Structure-Activity Relationship; Triazines

2013
PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.
    Journal of medicinal chemistry, 2016, Aug-11, Volume: 59, Issue:15

    Topics: Databases, Protein; Dose-Response Relationship, Drug; Drug Design; Humans; Ligands; Models, Molecular; Molecular Structure; Phosphodiesterase Inhibitors; Phosphoric Diester Hydrolases; Structure-Activity Relationship

2016
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, 2017, 01-01, Volume: 27, Issue:1

    Topics: Azepines; Cyclic Nucleotide Phosphodiesterases, Type 4; Dose-Response Relationship, Drug; Drug Design; Humans; Leukocytes, Mononuclear; Lipopolysaccharides; Molecular Structure; Phosphodiesterase 4 Inhibitors; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2017
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
    Journal of medicinal chemistry, 2019, 06-13, Volume: 62, Issue:11

    Topics: Animals; Caco-2 Cells; Catalytic Domain; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Drug Evaluation, Preclinical; Female; HEK293 Cells; Humans; Male; Mice; Models, Molecular; Phosphodiesterase 4 Inhibitors; Psoriasis; Rats; Stereoisomerism; Structure-Activity Relationship; Tetrahydroisoquinolines; Tissue Distribution

2019
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, 2020, Oct-15, Volume: 204

    Topics: Animals; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Drug Design; Enzyme Inhibitors; Humans; Hydrazones; Hypersensitivity; Lung; Male; Mice

2020
SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions.
    The Journal of pharmacology and experimental therapeutics, 1998, Volume: 284, Issue:1

    Topics: Animals; Anti-Inflammatory Agents; Cyclohexanecarboxylic Acids; Dose-Response Relationship, Drug; Female; Gastric Acid; Humans; In Vitro Techniques; Male; Nitriles; Phosphodiesterase Inhibitors; Pyrrolidinones; Rabbits; Rolipram

1998
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
    Journal of medicinal chemistry, 1998, Mar-12, Volume: 41, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Anti-Inflammatory Agents, Non-Steroidal; Binding, Competitive; Body Temperature; Brain; Bronchoconstriction; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Dogs; Gastric Acid; Guinea Pigs; Humans; Mice; Monocytes; Nitriles; Phosphodiesterase Inhibitors; Pyrrolidinones; Rabbits; Recombinant Proteins; Rolipram; Stereoisomerism; Structure-Activity Relationship; Tumor Necrosis Factor-alpha; Vomiting

1998
Effect of PDE4 inhibitors on zymosan-induced IL-8 release from human neutrophils: synergism with prostanoids and salbutamol.
    British journal of pharmacology, 1998, Volume: 123, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adult; Albuterol; Benzamides; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Drug Synergism; Humans; Interleukin-8; Neutrophils; Nitriles; Phosphodiesterase Inhibitors; Prostaglandins; Pyridines; Pyrrolidinones; Rolipram; Zymosan

1998
SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo.
    The Journal of pharmacology and experimental therapeutics, 1998, Volume: 287, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adoptive Transfer; Animals; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Humans; Interleukin-4; Male; Mice; Mice, Inbred Strains; Monocytes; Nitriles; Phosphodiesterase Inhibitors; Pyrrolidinones; Rolipram; Tumor Necrosis Factor-alpha

1998
Comparison of PDE 4 inhibitors, rolipram and SB 207499 (ariflo), in a rat model of pulmonary neutrophilia.
    Pulmonary pharmacology & therapeutics, 2001, Volume: 14, Issue:2

    Topics: Adrenalectomy; Animals; Cyclohexanecarboxylic Acids; Disease Models, Animal; Humans; Inflammation; Interleukin-1; Lung Diseases; Lung Diseases, Obstructive; Male; Neutrophils; Nitriles; Phosphodiesterase Inhibitors; Rats; Rats, Sprague-Dawley; Respiratory Distress Syndrome; Rolipram; Tumor Necrosis Factor-alpha

2001
Requirement of additional adenylate cyclase activation for the inhibition of human eosinophil degranulation by phosphodiesterase IV inhibitors.
    European journal of pharmacology, 2001, Apr-06, Volume: 417, Issue:1-2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adenylyl Cyclases; Adult; Albuterol; Benzamides; Cell Degranulation; Colforsin; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Dinoprostone; Dose-Response Relationship, Drug; Enzyme Activation; Eosinophil Peroxidase; Eosinophils; Histamine; Humans; Nitriles; Peroxidases; Phosphodiesterase Inhibitors; Pyridines; Rolipram; Superoxides; Theophylline

2001
Effects of inhibition of PDE4 and TNF-alpha on local and remote injuries following ischaemia and reperfusion injury.
    British journal of pharmacology, 2001, Volume: 134, Issue:5

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Capillary Permeability; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cytokines; Disease Models, Animal; Dose-Response Relationship, Drug; Immune Sera; Male; Neutrophils; Nitriles; Phosphodiesterase Inhibitors; Rats; Rats, Wistar; Reperfusion Injury; Rolipram; Survival Rate; Tumor Necrosis Factor-alpha

2001
Cyclic AMP-specific phosphodiesterase 4 inhibitors promote ABCA1 expression and cholesterol efflux.
    Biochemical and biophysical research communications, 2002, Jan-18, Volume: 290, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Apolipoprotein A-I; ATP Binding Cassette Transporter 1; ATP-Binding Cassette Transporters; Bronchodilator Agents; Carboxylic Acids; Cells, Cultured; Cholesterol; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Dose-Response Relationship, Drug; Gene Expression; Humans; Macrophages; Mice; Monocytes; Nitriles; Phosphodiesterase Inhibitors; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Rolipram

2002
Benefit of phosphodiesterase 4 inhibitors as supplemental therapy after lung transplantation concerning their antiproliferative effects: an experimental study using a heterotopic rodent model.
    Transplantation, 2002, Aug-15, Volume: 74, Issue:3

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclosporine; Graft Survival; Immunosuppressive Agents; Lung Transplantation; Nitriles; Phosphodiesterase Inhibitors; Rats; Rats, Inbred BN; Rats, Inbred Lew; Rolipram; Time Factors; Transplantation, Heterotopic; Transplantation, Homologous

2002
Anti-inflammatory and utero-relaxant effects in human myometrium of new generation phosphodiesterase 4 inhibitors.
    Biology of reproduction, 2004, Volume: 70, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Anti-Inflammatory Agents; Bronchodilator Agents; Carboxylic Acids; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Ethers; Female; Humans; Hydrocarbons, Fluorinated; In Vitro Techniques; Lipopolysaccharides; Myometrium; Nitriles; Phosphodiesterase Inhibitors; Pregnancy; Rolipram; Tumor Necrosis Factor-alpha; Uterine Contraction

2004
Modulation of matrix metalloproteinase production from human lung fibroblasts by type 4 phosphodiesterase inhibitors.
    Life sciences, 2004, Jul-02, Volume: 75, Issue:7

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Azepines; Blotting, Western; Bronchodilator Agents; Carboxylic Acids; Cell Line; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Drug Interactions; Drug Therapy, Combination; Fibroblasts; Humans; Isoenzymes; Lung; Matrix Metalloproteinase 1; Matrix Metalloproteinase 2; Metalloproteases; Niacinamide; Nitriles; Phosphodiesterase Inhibitors; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Rolipram; Tetradecanoylphorbol Acetate; Transforming Growth Factor beta; Transforming Growth Factor beta1; Tumor Necrosis Factor-alpha

2004
Role of PDE4 in superoxide anion generation through p44/42MAPK regulation: a cAMP and a PKA-independent mechanism.
    British journal of pharmacology, 2004, Volume: 143, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Bronchoalveolar Lavage Fluid; Bucladesine; CREB-Binding Protein; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Flavonoids; Gene Expression Regulation, Enzymologic; Imidazoles; Lipopolysaccharides; Macrophages; Mitogen-Activated Protein Kinases; N-Formylmethionine Leucyl-Phenylalanine; Neutrophils; Nitriles; Nuclear Proteins; p38 Mitogen-Activated Protein Kinases; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-raf; Pyridines; Rats; Rats, Wistar; Reactive Oxygen Species; Rolipram; Superoxides; Trans-Activators

2004
Potentiation and prolongation of long-term odor memory in neonate rats using a phosphodiesterase inhibitor.
    Neuroscience, 2005, Volume: 135, Issue:2

    Topics: Adrenergic beta-Agonists; Animals; Animals, Newborn; Behavior, Animal; Carboxylic Acids; Conditioning, Classical; Cyclohexanecarboxylic Acids; Discrimination Learning; Drug Interactions; Female; Isoproterenol; Male; Memory; Nitriles; Odorants; Phosphodiesterase Inhibitors; Rats; Rats, Sprague-Dawley; Rolipram; Time Factors

2005
Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors.
    Pulmonary pharmacology & therapeutics, 2006, Volume: 19, Issue:5

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Aminopyridines; Animals; Benzamides; Bronchial Spasm; Bronchoalveolar Lavage Fluid; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Disease Models, Animal; Immunization; Male; Neutrophils; Nitriles; Ovalbumin; Phosphodiesterase Inhibitors; Pneumonia; Pyridines; Rats; Respiratory Hypersensitivity; Rolipram; Serotonin; Treatment Outcome; Tumor Necrosis Factor-alpha

2006
Phosphodiesterase 4 inhibitors modulate beta2-adrenoceptor agonist-induced human airway hyperresponsiveness.
    Life sciences, 2006, Oct-12, Volume: 79, Issue:20

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adrenergic beta-2 Receptor Agonists; Adrenergic beta-Agonists; Bronchi; Bronchial Hyperreactivity; Carboxylic Acids; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Endothelin-1; Fenoterol; Humans; In Vitro Techniques; Muscle Contraction; Muscle, Smooth; Nitriles; Phosphodiesterase Inhibitors; Rolipram

2006
PDE4B5, a novel, super-short, brain-specific cAMP phosphodiesterase-4 variant whose isoform-specifying N-terminal region is identical to that of cAMP phosphodiesterase-4D6 (PDE4D6).
    The Journal of pharmacology and experimental therapeutics, 2007, Volume: 322, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Amino Acid Sequence; Animals; Base Sequence; Brain; Carboxylic Acids; Catalysis; Chlorocebus aethiops; Computational Biology; COS Cells; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Gene Expression; Humans; Isoenzymes; Lung; Mice; Molecular Sequence Data; Myocardium; Nerve Tissue Proteins; Nitriles; Oligonucleotide Array Sequence Analysis; Phosphodiesterase Inhibitors; Rolipram; Sequence Alignment; Transfection

2007
Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2007, Aug-15, Volume: 13, Issue:16

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Aminopyridines; Apoptosis; Benzamides; Carboxylic Acids; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Dexamethasone; Gene Expression Regulation, Leukemic; Hematopoietic System; Humans; Leukemia, Lymphocytic, Chronic, B-Cell; Nitriles; Phosphodiesterase Inhibitors; Receptors, Glucocorticoid; Rolipram

2007
Curative effects of phosphodiesterase 4 inhibitors cilomilast, roflumilast, and rolipram in dermatitis mouse model.
    Journal of dermatological science, 2008, Volume: 51, Issue:3

    Topics: Aminopyridines; Animals; Benzamides; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Dermatitis; Dermatitis, Contact; Disease Models, Animal; Eosinophil Peroxidase; Interleukin-4; Male; Mice; Mice, Inbred BALB C; Nitriles; Peroxidase; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Picryl Chloride; Rolipram

2008
Pharmacology of a novel, orally active PDE4 inhibitor.
    Pharmacology, 2009, Volume: 83, Issue:5

    Topics: Animals; Carboxylic Acids; Cell Line, Transformed; Cyclic AMP; Cyclohexanecarboxylic Acids; Disease Models, Animal; Dogs; Female; Guinea Pigs; Humans; Inflammation; Lymphocyte Activation; Male; Mice; Mice, Inbred BALB C; Nitriles; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Rats; Rats, Wistar; Rolipram; Tumor Necrosis Factor-alpha; Vomiting

2009
The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in
    The Journal of pharmacology and experimental therapeutics, 2009, Volume: 330, Issue:3

    Topics: Aminopyridines; Animals; Benzamides; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; Ferrets; Humans; Lipopolysaccharides; Mice; Mice, Inbred C57BL; Neutrophils; Nitriles; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Pica; Piperazines; Pyridines; Rats; Rats, Inbred Lew; Receptors, Adrenergic, alpha-2; Rolipram; Tumor Necrosis Factor-alpha; Vomiting

2009
Relationship between phosphodiesterase type 4 inhibition and anti-inflammatory activity of CI-1044 in rat airways.
    Fundamental & clinical pharmacology, 2010, Volume: 24, Issue:1

    Topics: Administration, Oral; Animals; Azepines; Carboxylic Acids; Cyclohexanecarboxylic Acids; Disease Models, Animal; Dose-Response Relationship, Drug; Drug Administration Schedule; Inflammation; Inhibitory Concentration 50; Lipopolysaccharides; Male; Niacinamide; Nitriles; Phosphodiesterase 4 Inhibitors; Phosphodiesterase Inhibitors; Pulmonary Eosinophilia; Rats; Rats, Inbred BN; Rolipram; Tumor Necrosis Factor-alpha

2010
Monitoring phosphodiesterase-4 inhibitors using liquid chromatography/(tandem) mass spectrometry in sports drug testing.
    Rapid communications in mass spectrometry : RCM, 2013, May-15, Volume: 27, Issue:9

    Topics: Aminopyridines; Benzamides; Chromatography, Liquid; Cyclohexanecarboxylic Acids; Cyclopropanes; Humans; Limit of Detection; Nitriles; Phosphodiesterase 4 Inhibitors; Rolipram; Spectrometry, Mass, Electrospray Ionization; Substance Abuse Detection; Tandem Mass Spectrometry

2013
Potentiation of long-acting β
    Respiratory research, 2021, Oct-19, Volume: 22, Issue:1

    Topics: Adrenergic beta-2 Receptor Agonists; Aminopyridines; Benzamides; Benzothiazoles; Budesonide; Cell Line; Chemokines; Cyclic AMP; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclohexanecarboxylic Acids; Cyclopropanes; Drug Synergism; Drug Therapy, Combination; Epithelial Cells; Formoterol Fumarate; Glucocorticoids; Humans; Lung; Multidrug Resistance-Associated Proteins; Nitriles; Phosphodiesterase 4 Inhibitors; Rolipram; Second Messenger Systems; Triazoles

2021
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
    Journal of medicinal chemistry, 2001, Aug-02, Volume: 44, Issue:16

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Enzyme Inhibitors; Humans; In Vitro Techniques; Magnetic Resonance Spectroscopy; Neutrophils; Phthalazines; Quantitative Structure-Activity Relationship; Regression Analysis; Rolipram; Stereoisomerism

2001
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, 2002, Jun-06, Volume: 45, Issue:12

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adamantane; Administration, Oral; Animals; Anti-Inflammatory Agents, Non-Steroidal; Cyclic Nucleotide Phosphodiesterases, Type 3; Cyclic Nucleotide Phosphodiesterases, Type 4; Cycloheptanes; Edema; Enzyme Inhibitors; Female; Humans; In Vitro Techniques; Leukocytes, Mononuclear; Lipopolysaccharides; Luminescent Measurements; Mice; Phthalazines; Reactive Oxygen Species; Structure-Activity Relationship; Tumor Necrosis Factor-alpha

2002
Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.
    Bioorganic & medicinal chemistry letters, 2012, Feb-15, Volume: 22, Issue:4

    Topics: Adrenergic beta-2 Receptor Agonists; Animals; Asthma; Drug Design; Guinea Pigs; Inhibitory Concentration 50; Molecular Structure; Phosphodiesterase 4 Inhibitors; Pulmonary Disease, Chronic Obstructive; Trachea

2012
Design, synthesis and evaluation of dual pharmacology β2-adrenoceptor agonists and PDE4 inhibitors.
    Bioorganic & medicinal chemistry letters, 2014, Jan-01, Volume: 24, Issue:1

    Topics: Adrenergic beta-2 Receptor Agonists; Cyclic Nucleotide Phosphodiesterases, Type 4; Dose-Response Relationship, Drug; Drug Design; Ethanolamines; Formoterol Fumarate; Humans; Molecular Structure; Phosphodiesterase 4 Inhibitors; Phthalazines; Receptors, Adrenergic, beta-2; Recombinant Proteins; Structure-Activity Relationship

2014