dihydropyridines and Airway-Obstruction

dihydropyridines has been researched along with Airway-Obstruction* in 1 studies

Other Studies

1 other study(ies) available for dihydropyridines and Airway-Obstruction

Article	Year
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 High-throughput file screening against inhibition of human lung PDE4 led to the discovery of 3-ethyl-1-(4-fluorophenyl)-6-phenyl-7-oxo-4, 5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine (11) as a novel PDE4 inhibitor. Subsequent SAR development, using an eosinophil PDE assay, led to analogues up to 50-fold more potent than 11 with IC50 values of 0.03-1.6 microM. One such compound, CP-220,629 (22) (IC50 = 0.44 microM), was efficacious in the guinea pig aerosolized antigen induced airway obstruction assay (ED50 2.0 mg/kg, po) and demonstrated a significant reduction in eosinophil (55%), neutrophil (65%), and IL-1beta (82%) responses to antigen challenge in atopic monkeys (10 mg/kg, po). 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

Article

Year

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

High-throughput file screening against inhibition of human lung PDE4 led to the discovery of 3-ethyl-1-(4-fluorophenyl)-6-phenyl-7-oxo-4, 5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine (11) as a novel PDE4 inhibitor. Subsequent SAR development, using an eosinophil PDE assay, led to analogues up to 50-fold more potent than 11 with IC50 values of 0.03-1.6 microM. One such compound, CP-220,629 (22) (IC50 = 0.44 microM), was efficacious in the guinea pig aerosolized antigen induced airway obstruction assay (ED50 2.0 mg/kg, po) and demonstrated a significant reduction in eosinophil (55%), neutrophil (65%), and IL-1beta (82%) responses to antigen challenge in atopic monkeys (10 mg/kg, po).

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