Abstract
New classes of de novo designed renin inhibitors are reported. Some of these compounds display excellent in vitro and in vivo activities toward human renin in a TGR model. The synthesis of these new types of mono- and bicyclic scaffolds are reported, and properties of selected compounds discussed.
MeSH terms
-
Bridged Bicyclo Compounds / chemistry
-
Bridged Bicyclo Compounds / classification*
-
Bridged Bicyclo Compounds / pharmacology*
-
Crystallography, X-Ray
-
Drug Design
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / classification*
-
Enzyme Inhibitors / pharmacology*
-
Humans
-
Models, Molecular
-
Molecular Structure
-
Renin / antagonists & inhibitors*
-
Stereoisomerism
-
Structure-Activity Relationship
Substances
-
Bridged Bicyclo Compounds
-
Enzyme Inhibitors
-
Renin