Design, synthesis and biological evaluation of novel trimethylpyrazine-2-carbonyloxy-cinnamic acids as potent cardiovascular agents

Autor:	Shouxun Wang, Peng Zhan, Hong Li, Guoning Li, Hongfei Chen, Xinyong Liu
Rok vydání:	2014
Předmět:	Pharmacology Organic Chemistry Pharmaceutical Science Biochemistry In vitro chemistry.chemical_compound Adenosine diphosphate Lipoic acid chemistry Drug Discovery Cardiovascular agent Molecular Medicine Potency Hydrogen peroxide IC50 EC50
Zdroj:	MedChemComm. 5:711
ISSN:	2040-2511 2040-2503
Popis:	A series of novel trimethylpyrazine-2-carbonyloxy-cinnamic acids and esters were designed, synthesized and evaluated for their inhibitory effect on adenosine diphosphate (ADP)-induced platelet aggregation in vitro and also assayed for their protective effect against hydrogen peroxide (H2O2)-induced oxidative damage on Ea.hy926 cells. The results showed that many compounds exhibited high activity in one or both of the assays, of which, compound F′10 displayed the highest protective effect on the proliferation of the damaged Ea.hy926 cells (EC50 = 1.7 μM), presenting almost 40 times higher potency than that of lipoic acid, and compound F3 was the most active anti-platelet aggregation agent with IC50 = 9.6 μM, comparable to that of clopidogrel. The structure–activity relationships of these compounds were also discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::11beda171e5558114d35816f52c86c16 https://doi.org/10.1039/c4md00022f Zobrazit plný text záznamu