2. Academic Validation
  3. Design, synthesis and biological evaluation of vortioxetine derivatives as new COX-1/2 inhibitors in human monocytes

Design, synthesis and biological evaluation of vortioxetine derivatives as new COX-1/2 inhibitors in human monocytes

  • Bioorg Med Chem. 2020 Dec 1;28(23):115760. doi: 10.1016/j.bmc.2020.115760.
Maria Talmon 1,  Raju D Chaudhari 2,  Hemant Suryavanshi 2,  Nilkanta Chowdhury 3,  Martina Quaregna 1,  Arianna Pin 1,  Angshuman Bagchi 3,  Goutam Biswas 4,  Luigia G Fresu 5
Affiliations

Affiliations

  • 1 Department of Health Sciences, School of Medicine, University of Piemonte Orientale, Via Solaroli, 17, 28100 Novara, Italy.
  • 2 Department of Chemistry, Cooch Behar Panchanan Barma University, Vivekananda Street, Cooch Behar 736101, West Bengal, India.
  • 3 Department of Biochemistry and Biophysics, University of Kalyani, Kalyani 741235, Nadia, West Bengal, India.
  • 4 Department of Chemistry, Cooch Behar Panchanan Barma University, Vivekananda Street, Cooch Behar 736101, West Bengal, India. Electronic address: goutam@cbpbu.ac.in.
  • 5 Department of Health Sciences, School of Medicine, University of Piemonte Orientale, Via Solaroli, 17, 28100 Novara, Italy. Electronic address: luigia.fresu@med.uniupo.it.
PMID: 32992247 DOI: 10.1016/j.bmc.2020.115760
Abstract

In order to identify a suitable alternative to non-steroidal anti-inflammatory drugs (NSAIDs) we aimed to develop derivatives of vortioxetine, a multimodal anti-depressive drug that has been shownpreviously to be endowed withanti-inflammatory activity in human monocytes/macrophages. Vortioxetine (1) was synthesized in good yield and different alkyl and aryl derivatives were prepared based on their structural diversity and easy availability. The compounds were tested on human monocytes isolated from healthy donors for theireffect on superoxide anion production and cytokine gene expression, and for COX-1/2 gene expression and activity modulation. Moreover, a docking study was performed to predict the interactions between the synthesized compounds and COX-1 and COX-2. Correlating experimental biological data to the molecular modelling studies, it emerged that among the novel compounds, 6 was endowed of antioxidant and anti-COX-1 activity, vortioxetine and 3 were good Antioxidants and mild anti-COX-1/2 inhibitors, while 7 was a good anti-COX-1/2 inhibitor and 11 was more specific versus COX-2.

Keywords

Human monocytes; Inflammation; NSAID; Vortioxetine.

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