226915-55-5Relevant academic research and scientific papers
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents
Chackalamannil, Samuel,Xia, Yan,Greenlee, William J.,Clasby, Martin,Doller, Darìo,Tsai, Hsingan,Asberom, Theodros,Czarniecki, Michael,Ahn, Ho-Sam,Boykow, George,Foster, Carolyn,Agans-Fantuzzi, Jacqueline,Bryant, Matthew,Lau, Janice,Chintala, Madhu
, p. 5884 - 5887 (2005)
Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in the binding assay, making it the most po
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists
Clasby, Martin C.,Chackalamannil, Samuel,Czarniecki, Michael,Doller, Dario,Eagen, Keith,Greenlee, William J.,Lin, Yan,Tsai, Hsingan,Xia, Yan,Ahn, Ho-Sam,Agans-Fantuzzi, Jacqueline,Boykow, George,Chintala, Madhu,Foster, Carolyn,Bryant, Matthew,Lau, Janice
, p. 1544 - 1548 (2007/10/03)
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 (IC50 = 6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.
THROMBIN RECEPTOR ANTAGONISTS
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Page 19, (2010/11/30)
Heterocyclic-substituted tricyclics of formula (I) or a pharmaceutically acceptable salt thereof, wherein: the single dotted line represents an optional double bond; the double dotted line represents an optional single bond; n is 0-2; Q is optionally subs
