| Literature DB >> 30771691 |
Alicia Jiménez-Almarza1, Daniel Diez-Iriepa2, Mourad Chioua3, Beatriz Chamorro4, Isabel Iriepa5, Ricardo Martínez-Murillo6, Dimitra Hadjipavlou-Litina7, María Jesús Oset-Gasque8, José Marco-Contelles9.
Abstract
In this work six PBN-related indanonitrones 1-6 have been designed, synthesized, and their neuroprotection capacity tested in vitro, under OGD conditions, in SH-SY5Y human neuroblastoma cell cultures. As a result, we have identified indanonitrones 1, 3 and 4 (EC50 = 6.64 ± 0.28 μM) as the most neuroprotective agents, and in particular, among them, indanonitrone 4 was also the most potent and balanced nitrone, showing antioxidant activity in three experiments [LOX (100 μM), APPH (51%), DPPH (36.5%)], being clearly more potent antioxidant agent than nitrone PBN. Consequently, we have identified (Z)-5-hydroxy-N-methyl-2,3-dihydro-1H-inden-1-imine oxide (4) as a hit-molecule for further investigation.Entities:
Keywords: Antioxidant; Indanonitrones; Lipid peroxidation; Lipoxygenase inhibitors; Neuroprotection; PBN; Synthesis
Year: 2019 PMID: 30771691 DOI: 10.1016/j.bioorg.2019.01.071
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275