Abstract
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.
2010 Elsevier Ltd. All rights reserved.
MeSH terms
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Cyclic Nucleotide Phosphodiesterases, Type 4 / metabolism*
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Humans
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Indolizines / chemistry*
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Indolizines / pharmacology*
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Phosphodiesterase 4 Inhibitors*
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Phosphodiesterase Inhibitors / chemistry*
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Phosphodiesterase Inhibitors / pharmacology*
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Structure-Activity Relationship
Substances
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Indolizines
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Phosphodiesterase 4 Inhibitors
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Phosphodiesterase Inhibitors
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Cyclic Nucleotide Phosphodiesterases, Type 4