Abstract
The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable.
MeSH terms
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Adenosine Diphosphate / pharmacology
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Administration, Oral
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Combinatorial Chemistry Techniques
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Drug Design
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Fibrinolytic Agents / chemical synthesis*
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Fibrinolytic Agents / chemistry
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Fibrinolytic Agents / pharmacology*
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Humans
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Molecular Structure
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Platelet Aggregation / drug effects
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Purinergic P2 Receptor Antagonists*
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Receptors, Purinergic P2Y1
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Structure-Activity Relationship
Substances
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Fibrinolytic Agents
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P2RY1 protein, human
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Purinergic P2 Receptor Antagonists
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Receptors, Purinergic P2Y1
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Adenosine Diphosphate