Derivatives of 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid as novel fibrinogen receptor antagonists

• Published in: Medicinal chemistry (Shp-sariqah, United Arab Emirates) Vol. 5; no. 2; p. 158
• Main Authors: Malovichko, Olga L, Krysko, Andrei A, Kabanova, Tatyana A, Andronati, Sergei A, Grishkovets, Vladimir I, Kachala, Vadim V, Panov, Denis A
• Format: Journal Article
• Language: English
• Published: Netherlands 01-03-2009
• Subjects: Blood Platelets - drug effects; Blood Platelets - metabolism; Fibrinogen - metabolism; Humans; Magnetic Resonance Spectroscopy; Molecular Structure; Oligopeptides - antagonists & inhibitors; Platelet Aggregation - drug effects; Platelet Glycoprotein GPIIb-IIIa Complex - metabolism; Platelet-Rich Plasma - drug effects; Protein Binding - drug effects; Receptors, Fibrinogen - antagonists & inhibitors; Receptors, Fibrinogen - metabolism; Tetrahydroisoquinolines - chemical synthesis; Tetrahydroisoquinolines - chemistry; Tetrahydroisoquinolines - pharmacology
• ISSN: 1573-4064
• DOI: 10.2174/157340609787582909

It has been proposed a novel method for obtaining of 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid as Arg-mimetic within the framework of search for novel fibrinogen receptor antagonists. New alpha (IIb)beta(3) antagonists were prepared on a base of 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid. Their high antiaggregatory activities in a human platelet rich plasma and ability to block FITC-Fg binding to alpha (IIb)beta(3) on washed human platelets were estimated.