Derivatives of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids as novel fibrinogen receptor antagonists

The synthesis of the novel fibrinogen receptor antagonists 9a– 9h is reported. The novel fibrinogen receptor antagonists containing fragments of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids were synthesized and successfully tested for their ability to inhibit platelet aggregation in...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5294-5297
Hauptverfasser:	Malovichko, Olga L., Petrus, Anna S., Krysko, Andrei A., Kabanova, Tatyana A., Andronati, Sergei A., Karaseva, Tamara L., Kiriyak, Anna V.
Format:	Artikel
Sprache:	eng
Schlagworte:	1,2,3,4-Tetrahydroisoquinoline Binding, Competitive - drug effects Biological and medical sciences Biological Assay Blood. Blood coagulation. Reticuloendothelial system Drug Evaluation, Preclinical Fibrinogen receptor antagonists Humans Medical sciences Molecular Mimicry Molecular Structure Pharmacology. Drug treatments Phthalic Acids - chemical synthesis Phthalic Acids - chemistry Phthalic Acids - pharmacology Platelet aggregation Platelet Aggregation - drug effects Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - pharmacology Platelet Glycoprotein GPIIb-IIIa Complex - drug effects Protein Binding - drug effects Receptors, Fibrinogen - antagonists & inhibitors RGD mimetics Stereoisomerism Structure-Activity Relationship α IIbβ 3
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Zusammenfassung:	The synthesis of the novel fibrinogen receptor antagonists 9a– 9h is reported. The novel fibrinogen receptor antagonists containing fragments of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids were synthesized and successfully tested for their ability to inhibit platelet aggregation in vitro and to block FITC-Fg binding to α IIbβ 3 on washed human platelets.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.07.090