Abstract
High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar analog from this series was shown to inhibit platelet aggregation.
MeSH terms
-
Aminoquinolines / chemical synthesis*
-
Aminoquinolines / chemistry
-
Aminoquinolines / pharmacology*
-
Combinatorial Chemistry Techniques
-
Humans
-
Molecular Structure
-
Platelet Aggregation Inhibitors / chemical synthesis*
-
Platelet Aggregation Inhibitors / chemistry
-
Platelet Aggregation Inhibitors / pharmacology*
-
Purinergic P2 Receptor Antagonists*
-
Receptors, Purinergic P2 / metabolism
-
Receptors, Purinergic P2Y1
-
Stereoisomerism
-
Structure-Activity Relationship
-
Thrombosis / drug therapy
Substances
-
1,2,3,4-tetrahydro-4-quinolinamine
-
Aminoquinolines
-
P2RY1 protein, human
-
Platelet Aggregation Inhibitors
-
Purinergic P2 Receptor Antagonists
-
Receptors, Purinergic P2
-
Receptors, Purinergic P2Y1