Abstract
A series of N-pyrimidinylpyrroloquinolones were discovered as extremely potent and selective PDE5 inhibitors. Representative compounds demonstrated in vivo efficacy in dog erectile dysfunction models and are orally bioavailable.
MeSH terms
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3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
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Administration, Oral
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Animals
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Biological Availability
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Cyclic Nucleotide Phosphodiesterases, Type 5
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Dogs
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Erectile Dysfunction / drug therapy*
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Male
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Quinolones / chemical synthesis*
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Quinolones / chemistry
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Quinolones / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Quinolones
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3',5'-Cyclic-GMP Phosphodiesterases
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Cyclic Nucleotide Phosphodiesterases, Type 5
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Pde5a protein, rat