Title of article
Design and synthesis of potent and selective macrocyclic thrombin inhibitors
Author/Authors
Philippe G. Nantermet، نويسنده , , James C. Barrow، نويسنده , , Christina L. Newton، نويسنده , , Janetta M. Pellicore، نويسنده , , MaryBeth Young، نويسنده , , S. Dale Lewis، نويسنده , , Bobby J. Lucas Jr.، نويسنده , , Julie A. Krueger، نويسنده , , Daniel R. McMasters، نويسنده , , Youwei Yan، نويسنده , , Lawrence C. Kuo، نويسنده , , Joseph P. Vacca، نويسنده , , Harold G. Selnick، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2003
Pages
4
From page
2781
To page
2784
Abstract
A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. Detailed SAR studies led to the incorporation of specific functional groups in the tether that enhanced functional activity against thrombin and provided exquisite selectivity against trypsin and tPA. X-ray crystallography and molecular modeling studies revealed the inhibitor-enzyme interactions responsible for this selectivity.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2003
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793447
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