New Inhibitors of Thrombin and Other Trypsin-like Proteases:  Hydrogen Bonding of an Aromatic Cyano Group with a Backbone Amide of the P1 Binding Site Replaces Binding of a Basic Side Chain

Highly effective thrombin inhibitors have been obtained by preparing boronic acid analogues of m-cyano-substituted phenylalanine and its incorporation into peptides. The cyano group enhances binding by several orders of magnitude. For example, Ac-(d)Phe-Pro-boroPheOH binds to thrombin with a K i of...

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