547755-67-9Relevant academic research and scientific papers
Design and synthesis of potent and selective macrocyclic thrombin inhibitors
Nantermet, Philippe G.,Barrow, James C.,Newton, Christina L.,Pellicore, Janetta M.,Young, MaryBeth,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,McMasters, Daniel R.,Yan, Youwei,Kuo, Lawrence C.,Vacca, Joseph P.,Selnick, Harold G.
, p. 2781 - 2784 (2007/10/03)
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.
Potent thrombin inhibitors via a 20-membered ring olefin metathesis macrocyclization
Nantermet, Philippe G.,Selnick, Harold G.
, p. 2401 - 2404 (2007/10/03)
Twenty-membered ring pyrazinone derived macrocycles were prepared as a means to enhance the potency of existing thrombin inhibitors. Macrocyclization was accomplished via Grubbs olefin metathesis of a highly functionalized allyl-alloc scaffold, thus furth
