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N-(Phenoxyalkyl)amides as MT1 and MT2 ligands: Antioxidant properties and inhibition of Ca2+/CaM-dependent kinase II

  作者 CAROCCI ALESSIA; CATALANO ALESSIA; BRUNO CLAUDIO; LOVECE ANGELO; ROSELLI MARIA GRAZIA; CAVALLUZZI MARIA MADDALENA; DE SANTIS FRANCESCO; DE PALMA ANNALISA; RUSCIANO MARIA ROSARIA; ILLARIO MADDALENA; FRANCHINI CARLO; LENTINI GIOVANNI  
  选自 期刊  Bioorganic & Medicinal Chemistry;  卷期  2013年21-4;  页码  847-851  
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[摘要]Recently a series of chiral N-(phenoxyalkyl)amides have been reported as potent MT1 and MT2 melatonergic ligands. Some of these compounds were selected and tested for their antioxidant properties by measuring their reducing effect against oxidation of 2',7'-dichlorodihydrofluorescein (DCFH) in the DCFH-diacetate (DCFH-DA) assay. Among the tested compounds, N-[2-(3-methoxyphenoxy)propyl]butanamide displayed potent antioxidant activity that was stereoselective, the (R)-enantiomer performing as the eutomer. This compound displayed strong cytoprotective activity against H2O2-induced cytotoxicity resulting slightly more active than melatonin, and performed as Ca2+/calmodulin-dependent kinase II (CaMKII) inhibitor, too. (C) 2012 Elsevier Ltd. All rights reserved.

 
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