Two series of new PAR1 antagonists have been identified. The first incorporates a cinnamoylpiperidine motif and the second a cinnamoylpyridine pattern. The synthesis, biological activity and structure–activity relationship of these compounds are presented. In each series, one analog showed potent in vivo antithrombotic activity in a rat AV shunt model, with up to 53% inhibition at 1.25 mpk iv for compound 30.
[Berini, Christophe; Winkelmann, Ole H.; Otten, Jennifer; Vicic, David A.; Navarro, Oscar Chemistry - A European Journal, 2010 , vol. 16, # 23 p. 6857 - 6860]
