Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets.

Young SE, Duvernay MT, Schulte ML, Lindsley CW, Hamm HE
PLoS One. 2013 8 (6): e65528

PMID: 23776495 · PMCID: PMC3679140 · DOI:10.1371/journal.pone.0065528

Protease activated receptor-4 (PAR4) is one of the thrombin receptors on human platelets and is a potential target for the management of thrombotic disorders. We sought to develop potent, selective, and novel PAR4 antagonists to test the role of PAR4 in thrombosis and hemostasis. Development of an expedient three-step synthetic route to access a novel series of indole-based PAR4 antagonists also necessitated the development of a platelet based high-throughput screening assay. Screening and subsequent structure activity relationship analysis yielded several selective PAR4 antagonists as well as possible new scaffolds for future antagonist development.

MeSH Terms (10)

Adult Blood Platelets Female Fibrinolytic Agents Humans Indazoles Indoles Male Platelet Activation Receptors, Thrombin

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