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Antioxidants (Basel). 2021 Oct 09;10(10). doi: 10.3390/antiox10101584.

1,5-Benzodiazepin-2(3H)-ones: In Vitro Evaluation as Antiparkinsonian Agents.

Antioxidants (Basel, Switzerland)

Ana Ortíz de Zárate, Marta Pérez-Torralba, Iñigo Bonet Isidro, Concepción López, Rosa M Claramunt, Diana Martínez-Casanova, Isabel Sánchez-Vera, Jesús Jiménez-González, José Luis Lavandera

Affiliations

  1. Instituto de Medicina Molecular Aplicada (IMMA), Facultad de Medicina, Universidad San Pablo-CEU, CEU Universities, Campus de Montepríncipe, E-28668 Madrid, Spain.
  2. Departamento de Química Orgánica y Bio-Orgánica, Facultad de Ciencias, Universidad Nacional de Educación a Distancia (UNED), Paseo Senda del Rey 9, E-28040 Madrid, Spain.
  3. Department of Pharmacology, Physiology and Neuroscience, Medical School, Rutgers, The State University of New Jersey, 185 South Orange Avenue, Newark, NJ 07103, USA.

PMID: 34679721 PMCID: PMC8533176 DOI: 10.3390/antiox10101584

Abstract

A new series of twenty-three 1,5-benzodiazepin-2(3H)-ones were synthesized and evaluated in the 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS), ferric reducing antioxidant power (FRAP), and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays as a new chemotype with antioxidant and good drug-like properties. All of the derivatives showed low cytotoxicity in comparison to curcumin against the human neuroblastoma SH-SY5Y and the human hepatoma HepG2 cell lines. Experimental solubility in bio-relevant media showed a good relationship with melting points in this series. Five compounds with the best antioxidant properties showed neuroprotectant activity against H

Keywords: 1,5-Benzodiazepin-2(3H)-ones; 6-OHD; MPP+; Parkinson disease; antioxidant; drug-like properties; mitochondrial dysfunction; neurodegeneration; neuroprotectant; oxidative stress

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