N-(Phenoxyalkyl)amides as MT(1) and MT(2) ligands: antioxidant properties and inhibition of Ca(2+)/CaM-dependent kinase II.

Autor: Carocci A; Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy. alessia.carocci@uniba.it, Catalano A, Bruno C, Lovece A, Roselli MG, Cavalluzzi MM, De Santis F, De Palma A, Rusciano MR, Illario M, Franchini C, Lentini G
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2013 Feb 15; Vol. 21 (4), pp. 847-51. Date of Electronic Publication: 2012 Dec 23.
DOI: 10.1016/j.bmc.2012.12.017
Abstrakt: Recently a series of chiral N-(phenoxyalkyl)amides have been reported as potent MT(1) and MT(2) 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 H(2)O(2)-induced cytotoxicity resulting slightly more active than melatonin, and performed as Ca(2+)/calmodulin-dependent kinase II (CaMKII) inhibitor, too.
(Copyright © 2012 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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