SERINE PROTEASE INHIBITORS

摘要

PURPOSE: Bifunctional serine protease inhibitors and methods of preparing boron-containing peptides are provided. CONSTITUTION: Serine protease inhibitors comprise a catalytic site directed moiety, which binds to and inhibits the active site of a serine protease, and an exosite associating moiety, which are joined by a connector moiety. The catalytic site directed moiety and the exosite associating moiety are capable of binding simultaneously to a molecule of the serine protease. A method of serine protease inhibitors comprises the following steps: (a) providing a solid phase having coupled thereto functional groups capable of reacting with an amino group or preferably with a carboxyl group or a reactive derivative thereof; (b) causing the amino or carboxyl group of a terminal amino acid of an amino acid sequence of a compound selectively to react with functional group; (c) coupling the amino acid sequentially preceding amino acid coupled to the solid phase to preceding amino acid; (d) repeating step (c) as often as necessary.