Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.

Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.
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DOI:
10.1016/j.bmcl.2004.09.002
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发表时间:
2004-11
影响因子:
2.7
通讯作者:
A. Krysko;B. M. Chugunov;O. L. Malovichko;S. Andronati;T. A. Kabanova;T. Karaseva;A. V. Kiriyak
A. Krysko;B. M. Chugunov;O. L. Malovichko;S. Andronati;T. A. Kabanova;T. Karaseva;A. V. Kiriyak
中科院分区:
医学4区
文献类型:
--
作者:
A. Krysko;B. M. Chugunov;O. L. Malovichko;S. Andronati;T. A. Kabanova;T. Karaseva;A. V. Kiriyak

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用4-(异吲哚-5-基)氨基-4-氧丁酸代替Arg-Gly基序合成了新型RGDF模拟物9a和9b。在体外实验中,所合成的化合物显示出抑制血小板聚集和阻断FITC-Fg与水洗人血小板α iib β3结合的高效能。
The novel RGDF mimetics 9a and 9b were synthesized with the use of 4-(isoindoline-5-yl)amino-4-oxobutyric acid as a 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 αIIbβ3on washed human platelets.