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Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.

Martin C Clasby,Samuel Chackalamannil,Michael Czarniecki,Dario Doller,Keith Eagen,William J Greenlee,Yan Lin,Hsingan Tsai,Yan Xia,Ho-Sam Ahn,Jacqueline Agans-Fantuzzi,George Boykow,Madhu Chintala,Carolyn Foster,Matthew Bryant,Janice Lau

Bioorganic & medicinal chemistry letters（2006）

Cited 28|Views37
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Abstract
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 (IC(50)=6.3 nM), a related compound 36 showing efficacy in a monkey ex vivo study.
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