Exploration of a new series of PAR1 antagonists

…, M Lamothe, C Maraval, C Horn, B Le Grand…

Index: Planty, Bruno; Pujol, Chantal; Lamothe, Marie; Maraval, Catherine; Horn, Clemens; Grand, Bruno Le; Perez, Michel Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 5 p. 1735 - 1739

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Citation Number: 16

Abstract

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.

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