Novel fibrinogen receptor antagonists--RGDF mimetics, 4-(1,2,3,4-tetrahydro-isoquinoline-7-yl)amino-4-oxo-butyric acid derivatives.
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 alphaIIbbeta3 on washed human platelets.
Krysko
Andrei A
AA
Department of Medicinal Chemistry, A V Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine, Odessa. peptides@paco.net
Malovichko
Olga L
OL
Andronati
Sergei A
SA
Kabanova
Tatyana A
TA
Karaseva
Tamara L
TL
Petrus
Anna S
AS
D007546:Isoquinolines; D009682:Magnetic Resonance Spectroscopy; D039341:Receptors, Fibrinogen / Q000037:antagonists & inhibitors*; D016339:Spectrometry, Mass, Fast Atom Bombardment
C514467:4-(1,2,3,4-tetrahydro-isoquinoline-7-yl)amino-4-oxo-butyric acid; D007546:Isoquinolines; D039341:Receptors, Fibrinogen