Abstract
The SAR of a series of beta-carboline derived type 5 phosphodiesterase inhibitors has been explored and we have discovered compounds with excellent levels of PDE5 potency and selectivity over PDE6. However, the series exhibits low levels of selectivity over PDE11, a phosphodiesterase with unknown function.
MeSH terms
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3',5'-Cyclic-GMP Phosphodiesterases
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Animals
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Benzene Derivatives / chemistry
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Benzene Derivatives / pharmacology
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Carbolines / chemical synthesis*
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Carbolines / chemistry
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Carbolines / pharmacology*
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Cattle
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Cyclic Nucleotide Phosphodiesterases, Type 5
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Dogs
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Drug Design
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Humans
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Inhibitory Concentration 50
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Isoenzymes
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Phosphodiesterase Inhibitors / chemical synthesis*
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Phosphodiesterase Inhibitors / chemistry
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Phosphodiesterase Inhibitors / pharmacology*
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Phosphoric Diester Hydrolases / metabolism*
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacology
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Recombinant Proteins / antagonists & inhibitors
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Spodoptera
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Structure-Activity Relationship
Substances
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Benzene Derivatives
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Carbolines
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Isoenzymes
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Phosphodiesterase Inhibitors
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Pyrrolidines
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Recombinant Proteins
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Phosphoric Diester Hydrolases
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3',5'-Cyclic-GMP Phosphodiesterases
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Cyclic Nucleotide Phosphodiesterases, Type 5
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PDE5A protein, human