Abstract
A novel class of potent and selective alpha-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known alpha-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described.
MeSH terms
-
Acetamides / chemistry
-
Acetamides / pharmacokinetics
-
Acetamides / pharmacology*
-
Adrenergic alpha-1 Receptor Antagonists*
-
Adrenergic alpha-Antagonists / chemistry
-
Adrenergic alpha-Antagonists / pharmacokinetics
-
Adrenergic alpha-Antagonists / pharmacology*
-
Animals
-
Chromatography, High Pressure Liquid
-
Dogs
-
Structure-Activity Relationship
Substances
-
Acetamides
-
Adrenergic alpha-1 Receptor Antagonists
-
Adrenergic alpha-Antagonists