Ligustrazine Derivatives. Part 6: Design, Synthesis and Evaluation of Novel Ligustrazinyl Acylguanidine Derivatives as Potential Cardiovascular Agents
| Autor: | Shouxun Wang, Fang Yu, Zhenyu Li, Xinyong Liu, Yuemao Shen, Lei Cui, Peng Zhan |
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| Rok vydání: | 2012 |
| Předmět: |
Cell Survival
Chemistry Stereochemistry Endothelial Cells Cardiovascular Agents Pharmacology Guanidines Antioxidants Cell Line Endothelial stem cell Inhibitory Concentration 50 Structure-Activity Relationship Design synthesis Cell culture Drug Design Pyrazines Drug Discovery Cardiovascular agent Humans Structure–activity relationship Inhibitory concentration 50 Cell Proliferation |
| Zdroj: | Medicinal Chemistry. 8:928-933 |
| ISSN: | 1573-4064 |
| Popis: | A series of novel Ligustrazinyl acylguanidines was designed, synthesized and evaluated for their protective effect on injured vascular endothelial cell (ECV-304). The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured endothelial cell. Among the active compounds, compounds 8b, 8f and 8l displayed remarkable antioxidative activity with low EC(50) values of 0.097, 0.059 and 0.094 mM, respectively. Structure-activity relationships were briefly discussed. |
| Databáze: | OpenAIRE |
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