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

被引：33

作者：

Carocci, Alessia ^{[1
]}

Catalano, Alessia ^{[1
]}

Bruno, Claudio ^{[1
]}

Lovece, Angelo ^{[1
]}

Roselli, Maria Grazia ^{[1
]}

Cavalluzzi, Maria Maddalena ^{[1
]}

De Santis, Francesco ^{[2
]}

De Palma, Annalisa ^{[2
]}

Rusciano, Maria Rosaria ^{[3
]}

Illario, Maddalena ^{[3
]}

Franchini, Carlo ^{[1
]}

Lentini, Giovanni ^{[1
]}

机构：

[1] Univ Bari Aldo Moro, Dipartimento Farm Sci Farmaco, I-70125 Bari, Italy

[2] Univ Bari Aldo Moro, Dipartimento Biosci Biotecnol & Biofarmaceut, I-70125 Bari, Italy

[3] Univ Naples Federico II, Dipartimento Biol & Patol Cellulare & Mol, I-80131 Naples, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 04期

关键词：

Antioxidants; Melatonin; CaMKII; DCFH-DA; DEPENDENT PROTEIN-KINASE; MELATONIN RECEPTORS; EXOGENOUS MELATONIN; PINEAL-GLAND; DYSFUNCTION; ENZYMES; SYSTEM; INVOLVEMENT; AGONISTS; THERAPY;

D O I：

10.1016/j.bmc.2012.12.017

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

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.

引用

页码：847 / 851

页数：5

共 46 条

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