Abstract
Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile dysfunction (MED) with a lower incidence of PDE-associated adverse effects. This paper describes the discovery of 14, a PDE5 inhibitor with improved potency and selectivity in vitro compared to sildenafil. This compound shows activity in a functional assay of erectile function comparable to that of sildenafil.
MeSH terms
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3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
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Animals
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Cyclic Nucleotide Phosphodiesterases, Type 5
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Erectile Dysfunction / drug therapy*
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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In Vitro Techniques
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Male
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Penis / drug effects*
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Penis / physiology
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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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Piperazines / pharmacology
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Purines
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Purinones / chemistry
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Quinazolines / chemical synthesis*
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Quinazolines / chemistry
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Quinazolines / pharmacology
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Rabbits
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Sildenafil Citrate
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Structure-Activity Relationship
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Sulfones
Substances
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1-(3-(1-((4-fluorophenyl)methyl)-7,8-dihydro-8-oxo-1H-imidazo(4,5-g)quinazolin-6-yl)-4-propoxyphenyl)carboxamide
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Imidazoles
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Phosphodiesterase Inhibitors
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Piperazines
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Purines
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Purinones
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Quinazolines
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Sulfones
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Sildenafil Citrate
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3',5'-Cyclic-GMP Phosphodiesterases
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Cyclic Nucleotide Phosphodiesterases, Type 5
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zaprinast