Synthesis of indole derived protease-activated receptor 4 antagonists and characterization in human platelets.
basic_science · Level V
Where this comes from
- Record sourced from PubMed, PMID 23776495.
- Also identified by DOI 10.1371/journal.pone.0065528 and PMC identifier 3679140.
- Licence recorded as CC BY.
- The licence permits redistribution, so the abstract is shown in full and the full text is available from the publisher.
Abstract
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.
Medical subject headings
- Blood Platelets
- Indazoles
- Indoles
- Receptors, Thrombin