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.
Planty, Bruno,Pujol, Chantal,Lamothe, Marie,Maraval, Catherine,Horn, Clemens,Grand, Bruno Le,Perez, Michel
scheme or table
p. 1735 - 1739
(2010/07/08)
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