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Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications
Y St-Denis1, C E Augelli-Szafran, B Bachand
1BioChem Therapeutic Inc., Laval, Québec, Canada.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.