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Discovery and SAR of small molecule PAR1 antagonists

I Rilatt, E Mirabel, B Le Grand, M Perez

文献索引:Rilatt, Ian; Mirabel, Etienne; Grand, Bruno Le; Perez, Michel Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 903 - 906

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被引用次数: 7

摘要

High-throughput screening resulted in the identification of a small molecule inhibitor of PAR1. Optimisation of the initial hit led to the discovery of compounds 34 and 49, which displayed antithrombotic activity in an arteriovenous shunt model in the rat after iv ...