Title: Novel Fibrinogen Receptor Antagonists - RGDF Mimetics, 4-(1,2,3,4- tetrahydro-isoquinoline-7-yl)amino-4-oxo-butyric Acid Derivatives
VOLUME: 2 ISSUE: 3
Author(s):Sergei A. Andronati, Olga L. Malovichko, Andrei A. Krysko, Tatyana A. Kabanova, Tamara L. Karaseva and Anna S. Petrus
Affiliation:Department of MedicinalChemistry, A.V. Bogatsky Physico-Chemical Institute of the NationalAcademy of Sciences of Ukraine. 86 Lustdorfskaya doroga, 65080, Odessa,Ukraine.
Keywords:Fibrinogen receptor antagonists, αIIbβ3, GP IIb/IIIa, RGD mimetics, 1,2,3,4-tetrahydro-isoquinoline, platelet aggregation
Abstract: Two novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydro-isoquinoline-7-yl)amino-4- oxo-butyric acid as a new surrogate of Arg-Gly motif. The synthesized compounds have demonstrated a high potency to inhibit platelet aggregation in vitro and to block FITC-Fg binding to αIIbβ3 on washed human platelets.