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

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

  • Bioorg Med Chem. 2013 Feb 15;21(4):847-51. doi: 10.1016/j.bmc.2012.12.017.
Alessia Carocci 1,  Alessia Catalano,  Claudio Bruno,  Angelo Lovece,  Maria Grazia Roselli,  Maria Maddalena Cavalluzzi,  Francesco De Santis,  Annalisa De Palma,  Maria Rosaria Rusciano,  Maddalena Illario,  Carlo Franchini,  Giovanni Lentini
Affiliations

Affiliation

  • 1 Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy. alessia.carocci@uniba.it
PMID: 23332368 DOI: 10.1016/j.bmc.2012.12.017
Abstract

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.

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