title: Discovery and SAR of small molecule PAR1 antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry 4, Centre de Recherche Pierre Fabre, 17 Avenue Jean Moulin, 81106 Castres Cedex, France. Ian.Rilatt@Pierre-Fabre.com
authors.forename: Ian
authors.initials: I
authors.lastname: Rilatt
authors.forename: Etienne
authors.initials: E
authors.lastname: Mirabel
authors.forename: Bruno
authors.initials: B
authors.lastname: Le Grand
authors.forename: Michel
authors.initials: M
authors.lastname: Perez
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D055808:Drug Discovery / Q000379:methods*; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000502:physiology; D009842:Oligopeptides / Q000737:chemistry* / Q000494:pharmacology*; D011480:Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D044463:Receptor, PAR-1 / Q000502:physiology; D013329:Structure-Activity Relationship; D010975:Platelet Aggregation Inhibitors
chemical_list: C090291:C186 65; D009842:Oligopeptides; D011480:Protease Inhibitors; D044463:Receptor, PAR-1; D010975:Platelet Aggregation Inhibitors