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Bioorg Med Chem Lett. 2010 Feb 1;20(3):903-6. doi: 10.1016/j.bmcl.2009.12.072. Epub 2009 Dec 23.

Discovery and SAR of small molecule PAR1 antagonists.

Author information

1
Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17 Avenue Jean Moulin, 81106 Castres Cedex, France. Ian.Rilatt@Pierre-Fabre.com

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.

PMID:
20042334
DOI:
10.1016/j.bmcl.2009.12.072
[Indexed for MEDLINE]

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