Derivatives of 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acid as novel fibrinogen receptor antagonists.
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.
Malovichko
Olga L
OL
Department of Medicinal Chemistry, A.V. Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine. 86 Lustdorfskaya doroga, 65080, Odessa, Ukraine.
Krysko
Andrei A
AA
Kabanova
Tatyana A
TA
Andronati
Sergei A
SA
Grishkovets
Vladimir I
VI
Kachala
Vadim V
VV
Panov
Denis A
DA
D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D005340:Fibrinogen / Q000378:metabolism; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D009842:Oligopeptides / Q000037:antagonists & inhibitors; D010974:Platelet Aggregation / Q000187:drug effects; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000378:metabolism; D053657:Platelet-Rich Plasma / Q000187:drug effects; D011485:Protein Binding / Q000187:drug effects; D039341:Receptors, Fibrinogen / Q000037:antagonists & inhibitors* / Q000378:metabolism; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
D009842:Oligopeptides; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D039341:Receptors, Fibrinogen; D044005:Tetrahydroisoquinolines; C047981:arginyl-glycyl-aspartic acid; D005340:Fibrinogen