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

Olga L Malovichko; Anna S Petrus; Andrei A Krysko; Tatyana A Kabanova; Sergei A Andronati; Tamara L Karaseva; Anna V Kiriyak

doi:10.1016/j.bmcl.2006.07.090

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

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5294-7. doi: 10.1016/j.bmcl.2006.07.090. Epub 2006 Aug 21.

Authors

Olga L Malovichko¹, Anna S Petrus, Andrei A Krysko, Tatyana A Kabanova, Sergei A Andronati, Tamara L Karaseva, Anna V Kiriyak

Affiliation

¹ Department of Medicinal Chemistry, A.V. Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine, 86 Lustdorfskaya doroga, 65080 Odessa, Ukraine.

PMID: 16919941
DOI: 10.1016/j.bmcl.2006.07.090

Abstract

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 alpha(IIb)beta(3) on washed human platelets.

MeSH terms

Binding, Competitive / drug effects
Biological Assay
Drug Evaluation, Preclinical
Humans
Molecular Mimicry
Molecular Structure
Phthalic Acids / chemical synthesis
Phthalic Acids / chemistry
Phthalic Acids / pharmacology*
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*
Stereoisomerism
Structure-Activity Relationship

Substances

Phthalic Acids
Platelet Aggregation Inhibitors
Platelet Glycoprotein GPIIb-IIIa Complex
Receptors, Fibrinogen
isophthalate