title: Derivatives of tetrahydroisoquinoline: synthesis and initial evaluation of novel non-peptide antagonists of the alpha(IIb)beta(3)-integrin.
abstract: The novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-4-oxobutyric or 5-(1,2,3,4-tetrahydroisoquinoline-7-yl)amino-5-oxopentanoic acids 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 alpha(IIb)beta(3) on washed human platelets.
authors.affiliation: Department of Medicinal Chemistry, A.V. Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine, Odessa, Ukraine. peptides@physchem.od.ua
authors.forename: Andrei A
authors.initials: AA
authors.lastname: Krysko
authors.forename: Olga L
authors.initials: OL
authors.lastname: Krysko
authors.forename: Tatyana A
authors.initials: TA
authors.lastname: Kabanova
authors.forename: Sergei A
authors.initials: SA
authors.lastname: Andronati
authors.forename: Vladimir M
authors.initials: VM
authors.lastname: Kabanov
mesh_terms: D005340:Fibrinogen / Q000737:chemistry; D016650:Fluorescein-5-isothiocyanate / Q000737:chemistry; D006801:Humans; D009842:Oligopeptides / Q000737:chemistry; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011485:Protein Binding; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D009842:Oligopeptides; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D044005:Tetrahydroisoquinolines; C084961:arginyl-glycyl-aspartyl-phenylalanine; C014843:1,2,3,4-tetrahydroisoquinoline; D005340:Fibrinogen; D016650:Fluorescein-5-isothiocyanate