Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrin αIIbβ3
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
26912112
DOI
10.1016/j.bmcl.2016.02.011
PII: S0960-894X(16)30114-7
Knihovny.cz E-resources
- Keywords
- 2-Piperazin-1-yl-quinazoline, Fibrinogen receptor antagonists, Platelet aggregation, α(IIb)β(3),
- MeSH
- Platelet Aggregation drug effects MeSH
- Quinazolines chemistry pharmacology MeSH
- Platelet Aggregation Inhibitors chemistry pharmacology MeSH
- Humans MeSH
- Ligands MeSH
- Piperazines chemistry pharmacology MeSH
- Molecular Docking Simulation MeSH
- Platelet Glycoprotein GPIIb-IIIa Complex metabolism MeSH
- Blood Platelets cytology drug effects metabolism MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Quinazolines MeSH
- Platelet Aggregation Inhibitors MeSH
- Ligands MeSH
- Piperazines MeSH
- Platelet Glycoprotein GPIIb-IIIa Complex MeSH
A series of 2-piperazin-1-yl-quinazolines were synthesized and evaluated for their antiaggregative activity. The synthesized small molecule compounds have potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to αIIbβ3 integrin in a suspension of washed human platelets. The key αIIbβ3 protein-ligand interactions were determined in docking experiments and some correlations have been observed between values of the affinity and docking scores.
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