Design and synthesis of amidino-tyrosine derivatives as non-peptide fibrinogen receptor antagonists

T L Xu; X T Jiang; W Y Hua; P Z Ni; Y M Pei

doi:10.1016/s0960-894x(99)00308-x

Design and synthesis of amidino-tyrosine derivatives as non-peptide fibrinogen receptor antagonists

Bioorg Med Chem Lett. 1999 Jul 19;9(14):1933-6. doi: 10.1016/s0960-894x(99)00308-x.

Authors

T L Xu¹, X T Jiang, W Y Hua, P Z Ni, Y M Pei

Affiliation

¹ Institute of Radiation Medicine, Beijing, PR, China.

PMID: 10450956
DOI: 10.1016/s0960-894x(99)00308-x

Abstract

The design, synthesis and antiaggregation activity of amidino-tyrosine derivatives based on Arg-Gly-Asp (RGD) tripeptide sequence as non-peptide fibrinogen receptor antagonists is described. Optimization of the spacer and the substituent at the C-terminal is reported.

MeSH terms

Adenosine Diphosphate / pharmacology
Drug Design
Inhibitory Concentration 50
Oligopeptides / chemistry
Platelet Aggregation Inhibitors / chemical synthesis*
Platelet Aggregation Inhibitors / pharmacology*
Platelet Glycoprotein GPIIb-IIIa Complex / antagonists & inhibitors*
Tyrosine / chemistry*

Substances

Oligopeptides
Platelet Aggregation Inhibitors
Platelet Glycoprotein GPIIb-IIIa Complex
Tyrosine
Adenosine Diphosphate
arginyl-glycyl-aspartic acid