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Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2013, Volume 23, Issue 1, pp. 375 - 381
(−)-6-(7-Methoxy-2-(trifluoromethyl)pyrazolo[1,5- ]pyridin-4-yl)-5-methyl-4,5-dihydropyridazin-3(2 )-one (KCA-1490) exhibits moderate dual PDE3/4-inhibitory... 
Phosphodiesterase (PDE) | Inhaled administration | Dual PDE3/4 inhibitor | Asthma | COPD | MORTALITY | CHRONIC HEART-FAILURE | BRONCHODILATORY ACTIVITY | DESIGN | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | 4,5-DIHYDRO-6-<4-(1H-IMIDAZOL-1-YL)PHENYL>-3(2H)-PYRIDAZINONES | OBSTRUCTIVE PULMONARY-DISEASE | POSITIVE INOTROPIC AGENTS | CORTICOSTEROIDS | CARDIOTONIC AGENTS | ROFLUMILAST | Cyclic Nucleotide Phosphodiesterases, Type 3 - chemistry | Phosphodiesterase 3 Inhibitors - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Pyridines - chemistry | Structure-Activity Relationship | Phosphodiesterase 4 Inhibitors - chemical synthesis | Bronchodilator Agents - chemistry | Drug Design | Bronchoalveolar Lavage Fluid - cytology | Cyclic Nucleotide Phosphodiesterases, Type 3 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Phosphodiesterase 4 Inhibitors - chemistry | Anti-Inflammatory Agents - pharmacology | Administration, Inhalation | Rats | Bronchodilator Agents - pharmacology | Bronchodilator Agents - chemical synthesis | Phosphodiesterase 4 Inhibitors - pharmacology | Pyridazines - chemistry | Phosphodiesterase 3 Inhibitors - chemical synthesis | Animals | Anti-Inflammatory Agents - chemistry | Protein Binding | Leukocytes - drug effects | Anti-Inflammatory Agents - chemical synthesis | Anti-inflammatory drugs | Respiratory agents
Journal Article
Journal Article
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 03/2012, Volume 20, Issue 5, pp. 1644 - 1658
(−)-6-(7-Methoxy-2-trifluoromethylpyrazolo[1,5- ]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2 )-pyridazinone (KCA-1490) is a dual PDE3/4 inhibitor that exhibits... 
Phosphodiesterase (PDE) | Fused bicyclic heteroaromatics | Dual PDE3/4 inhibitor | Asthma | COPD | CHEMISTRY, MEDICINAL | MANAGEMENT | RECEPTOR ANTAGONISTS | COMBINATION THERAPY | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | INHALED CORTICOSTEROIDS | CHEMISTRY, ORGANIC | OBSTRUCTIVE PULMONARY-DISEASE | SMOOTH-MUSCLE | POSITIVE INOTROPIC AGENTS | CARDIOTONIC AGENTS | Phosphodiesterase 4 Inhibitors - chemistry | Anti-Inflammatory Agents - pharmacology | Phosphodiesterase 3 Inhibitors - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Pyridines - chemistry | Bridged Bicyclo Compounds, Heterocyclic - chemistry | Humans | Pyridines - chemical synthesis | Models, Molecular | Bronchodilator Agents - pharmacology | Structure-Activity Relationship | Bronchodilator Agents - chemical synthesis | Phosphodiesterase 4 Inhibitors - pharmacology | Phosphodiesterase 4 Inhibitors - chemical synthesis | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Bronchodilator Agents - chemistry | Phosphodiesterase 3 Inhibitors - chemical synthesis | Anti-Inflammatory Agents - chemistry | Bronchoconstriction - drug effects | Drug Design | Anti-Inflammatory Agents - chemical synthesis | Pyridines - pharmacology | Bridged Bicyclo Compounds, Heterocyclic - chemical synthesis | Anti-inflammatory drugs | Lung diseases, Obstructive
Journal Article
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 09/2011, Volume 21, Issue 18, pp. 5451 - 5456
A structural survey of pyrazolopyridine-pyridazinone phosphodiesterase (PDE) inhibitors was made with a view to optimization of their dual PDE3/4-inhibitory... 
Ibudilast | PDE3 inhibitors | Cyclic 3′,5′-nucleotide phosphodiesterase (PDE) | Respiratory disease | PDE4 inhibitors | Cyclic 3',5'-nucleotide phosphodiesterase (PDE) | Cyclic 3 ',5 '-nucleotide phosphodiesterase (PDE) | CHRONIC HEART-FAILURE | SLOW REACTING SUBSTANCE | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | IDENTIFICATION | OBSTRUCTIVE PULMONARY-DISEASE | ASTHMA | POSITIVE INOTROPIC AGENTS | HIGHLY POTENT | CARDIOTONIC AGENTS | Phosphodiesterase 3 Inhibitors - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Pyrazoles - chemical synthesis | Pyridines - chemistry | Stereoisomerism | Anti-Inflammatory Agents, Non-Steroidal - chemistry | Structure-Activity Relationship | Phosphodiesterase 4 Inhibitors - chemical synthesis | Anti-Inflammatory Agents, Non-Steroidal - pharmacology | Dose-Response Relationship, Drug | Bronchodilator Agents - chemistry | Pyrazoles - chemistry | Drug Design | Molecular Structure | Cyclic Nucleotide Phosphodiesterases, Type 3 - metabolism | Anti-Inflammatory Agents, Non-Steroidal - chemical synthesis | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Drug Evaluation, Preclinical | Pyrazoles - pharmacology | Phosphodiesterase 4 Inhibitors - chemistry | Guinea Pigs | Pyridines - chemical synthesis | Rats | Bronchodilator Agents - pharmacology | Bronchodilator Agents - chemical synthesis | Phosphodiesterase 4 Inhibitors - pharmacology | Phosphodiesterase 3 Inhibitors - chemical synthesis | Animals | Pyridines - pharmacology | Anti-inflammatory drugs | Pyridine
Journal Article
Scientific Reports, ISSN 2045-2322, 12/2017, Volume 7, Issue 1, pp. 1917 - 11
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 2011, Volume 21, Issue 6, pp. 1617 - 1620
In this work, we tried to find a new scaffold for a PDE3 using virtual screening for the obesity treatment. We first analyzed structural features for the known... 
Virtual screening | Obesity | Inhibitor | PDE3 | POTENT | ENERGY | CHEMISTRY, MEDICINAL | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | CHEMISTRY, ORGANIC | GENE FAMILY | MECHANISMS | Animals | Phosphodiesterase 3 Inhibitors - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Adipocytes - metabolism | Humans | Models, Molecular | Mice | Molecular Structure | Drug Discovery
Journal Article
Organic & Biomolecular Chemistry, ISSN 1477-0520, 12/2016, Volume 14, Issue 48, pp. 11402 - 11414
Various N-fused isoquinoline derivatives were synthesized using a new one-pot reaction of 1-bromo-2-(2,2-difluorovinyl)benzenes with N-H group containing... 
Journal Article
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 02/2005, Volume 48, Issue 4, pp. 1237 - 1243
3-(3-Cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-adenine V11294 (1) has been identified as a lead structure, which selectively inhibits human lung PDE4 (436... 
ISOZYMES | FORMS | SITE | CHEMISTRY, MEDICINAL | AGENTS | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE | V11294 | CAMP | ROLIPRAM
Journal Article
Asian Journal of Chemistry, ISSN 0970-7077, 2011, Volume 23, Issue 9, pp. 4008 - 4010
The enzyme phosphodiesterase-4 (PDE4) plays a key role in many physiological or pathological processes in mammalian organs, where its inhibition increases... 
Mammalian organs | Cyclic adenosine monophosphate | Phosphodiesterase | SELECTIVE-INHIBITION | INDUCED TOXIC STRESS | SILDENAFIL | PROTECTION | THEOPHYLLINE | CHEMISTRY, MULTIDISCIPLINARY | SALIVA | INDUCED OXIDATIVE STRESS | TYPE-4 INHIBITORS | AGENTS | PENTOXIFYLLINE
Journal Article
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