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Phosphodiesterase inhibitors. Part 6: design, synthesis, and structure-activity relationships of PDE4-inhibitory pyrazolo[1,5-a]pyridines with anti-inflammatory activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2013 Oct 01; Vol. 23 (19), pp. 5311-6. Date of Electronic Publication: 2013 Aug 08. - Publication Year :
- 2013
-
Abstract
- We previously identified KCA-1490 [(-)-6-(7-methoxy-2-trifluoromethyl-pyrazolo[1,5-a]pyridin-4-yl)-5-methyl-4,5-dihydro-3-(2H)-pyridazinone], a dual PDE3/4 inhibitor. In the present study, we found highly potent selective PDE4 inhibitors derived from the structure of KCA-1490. Among them, N-(3,5-dichloropyridin-4-yl)-7-methoxy-2-(trifluoromethyl)pyrazolo[1,5-a]pyridine-4-carboxamide (2a) had good anti-inflammatory effects in an animal model.<br /> (Copyright © 2013 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Enzyme Activation drug effects
Inhibitory Concentration 50
Models, Animal
Molecular Structure
Pyrazoles chemistry
Pyrazoles pharmacology
Rats
Structure-Activity Relationship
Anti-Inflammatory Agents chemical synthesis
Anti-Inflammatory Agents chemistry
Anti-Inflammatory Agents pharmacology
Drug Design
Phosphodiesterase 4 Inhibitors chemical synthesis
Phosphodiesterase 4 Inhibitors chemistry
Phosphodiesterase 4 Inhibitors pharmacology
Pyrazoles chemical synthesis
Pyridines chemical synthesis
Pyridines chemistry
Pyridines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 23
- Issue :
- 19
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 23988356
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.07.069