Horst Juraszyk

New antithrombotic RGD-mimetics with high bioavailability

Abstract A new class of antithrombotic RGD-mimetics with a novel axazolidinonemethyl scaffold was synthesized. High oral activity and bioavailability was found in this series of compounds.

New peptidomimetics in the chemistry of fibrinogen receptor antagonists

RGD-peptidomimetics are currently being investigated as a class of potential antithrombotics that antagonize the fibrinogen receptor, GP IIb/IIIa, on the surface of platelets. These mimetics are expected to have decisive advantages-such as higher activity and specificity, oral bioavailability and longer duration of action-over known antithrombotics. For further optimization in this respect, novel peptidomimetic GP IIb/IIIa antagonists with an oxazolidinonemethyl central building block were synthesized. This building block proved to be very versatile as an ‘anchor’ for structurally different C-termini and was the starting point for highly efficient and orally active compounds.