Abstract
Efforts to improve the potency and physical properties of the aminopyridiopyrazinone class of PDE5 inhibitors through modification of the core ring system are described. Five new ring systems are evaluated and features that impart improved potency and improved solubility are delineated.
MeSH terms
-
Administration, Oral
-
Aminopyridines / chemical synthesis*
-
Aminopyridines / pharmacology
-
Animals
-
Chemistry, Pharmaceutical / methods
-
Cyclic GMP / chemistry
-
Cyclic Nucleotide Phosphodiesterases, Type 5 / chemistry
-
Drug Design
-
Humans
-
Hydrogen-Ion Concentration
-
Hypertension / drug therapy
-
Microsomes / drug effects
-
Models, Chemical
-
Phosphodiesterase 5 Inhibitors*
-
Phosphodiesterase Inhibitors / chemical synthesis*
-
Phosphodiesterase Inhibitors / pharmacology
-
Pyrazines / chemical synthesis*
-
Pyrazines / pharmacology
-
Rats
-
Rats, Sprague-Dawley
-
Solubility
Substances
-
Aminopyridines
-
Phosphodiesterase 5 Inhibitors
-
Phosphodiesterase Inhibitors
-
Pyrazines
-
Cyclic Nucleotide Phosphodiesterases, Type 5
-
Cyclic GMP