Abstract
The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.
MeSH terms
-
Animals
-
Blood Platelets / drug effects
-
Blood Platelets / metabolism
-
Fibrinolytic Agents / chemical synthesis*
-
Fibrinolytic Agents / chemistry
-
Fibrinolytic Agents / pharmacology
-
Heterocyclic Compounds, 3-Ring / chemical synthesis*
-
Heterocyclic Compounds, 3-Ring / chemistry
-
Heterocyclic Compounds, 3-Ring / pharmacology
-
Macaca fascicularis
-
Platelet Aggregation Inhibitors / chemical synthesis
-
Platelet Aggregation Inhibitors / chemistry
-
Platelet Aggregation Inhibitors / pharmacology
-
Pyridines / chemical synthesis*
-
Pyridines / chemistry
-
Pyridines / pharmacology
-
Quinolines / chemistry*
-
Receptor, PAR-1 / antagonists & inhibitors*
-
Receptors, Thrombin / metabolism
-
Structure-Activity Relationship
Substances
-
4-(5-(3-trifluoromethylphenyl)pyridin-2-yl)ethenyl-3-methyldecahydronaphtho(2,3-c)furan-1(3H)-one
-
Fibrinolytic Agents
-
Heterocyclic Compounds, 3-Ring
-
Platelet Aggregation Inhibitors
-
Pyridines
-
Quinolines
-
Receptor, PAR-1
-
Receptors, Thrombin
-
quinoline