Title of article
Discovery and initial structure–Activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists
Author/Authors
James C. Barrow، نويسنده , , Philippe G. Nantermet، نويسنده , , Harold G. Selnick، نويسنده , , Kristen L. Glass، نويسنده , , Phung L. Ngo، نويسنده , , Mary Beth Young، نويسنده , , Janetta M. Pellicore، نويسنده , , Michael J. Breslin، نويسنده , , John H. Hutchinson، نويسنده , , Roger M. Freidinger، نويسنده , , Cindra Condra، نويسنده , , Jerzy Karczewski، نويسنده , , Rodney A. Bednar، نويسنده , , Stanley L. Gaul، نويسنده , , Andrew Stern، نويسنده , , Robert Gould، نويسنده , , Thomas M. Connolly، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
6
From page
2691
To page
2696
Abstract
Thrombin is the most potent agonist of platelet activation, and its effects are predominantly mediated by platelet thrombin receptors. Therefore, antagonists of the thrombin receptor have potential utility for the treatment of thrombotic disorders. Screening of combinatorial libraries revealed 2 to be a potent antagonist of the thrombin receptor. Modifications of this structure produced 11k, which inhibits thrombin receptor stimulated secretion and aggregation of platelets.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791709
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