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

• Published in: Bioorganic & medicinal chemistry letters 2006-10, Vol.16 (20), p.5294-5297
• Main Authors: Malovichko, Olga L., Petrus, Anna S., Krysko, Andrei A., Kabanova, Tatyana A., Andronati, Sergei A., Karaseva, Tamara L., Kiriyak, Anna V.
• Format: Article
• Language: English
• Subjects: 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
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2006.07.090

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.