Discovery and SAR of small molecule PAR1 antagonists |
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| Authors: | Ian Rilatt Etienne Mirabel Bruno Le Grand Michel Perez |
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| Affiliation: | 1. Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin, 81106 Castres Cedex, France;2. Department of Cardiovascular Diseases 2, Centre de Recherche Pierre Fabre, 17, Avenue Jean Moulin, 81106 Castres Cedex, France |
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| Abstract: | 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 administration. |
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