Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors
| Autor: | Arlene Joan Dietrich, Warren D. Hirst, Paul Jeffrey Dollings, Afshin Ghavami, Kerri Lipinski, Andrew F. Donnell, John A. Butera |
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| Rok vydání: | 2010 |
| Předmět: |
Phosphodiesterase Inhibitors
Stereochemistry Chemistry Organic Chemistry Clinical Biochemistry High selectivity Indolizines Pharmaceutical Science Biochemistry Combinatorial chemistry Cyclic Nucleotide Phosphodiesterases Type 4 Structure-Activity Relationship PDE4B Drug Discovery Humans Molecular Medicine Identification (biology) Phosphodiesterase 4 Inhibitors Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 20:2163-2167 |
| ISSN: | 0960-894X |
| Popis: | Substituted pyridazino[4,5-b]indolizines were identified as potent and selective PDE4B inhibitors. We describe the structure-activity relationships generated around an HTS hit that led to a series of compounds with low nanomolar affinity for PDE4B and high selectivity over the PDE4D subtype. |
| Databáze: | OpenAIRE |
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