2. Academic Validation
  3. Stilbene-pyridazinone hybrids: design, synthesis and in vitro antiplatelet activity screening

Stilbene-pyridazinone hybrids: design, synthesis and in vitro antiplatelet activity screening

  • Bioorg Chem. 2024 Sep:150:107615. doi: 10.1016/j.bioorg.2024.107615.
Maria Carmen Costas-Lago 1,  Pedro Besada 1,  Ricardo Mosquera 2,  Ernesto Cano 3,  Carmen Terán 4
Affiliations

Affiliations

  • 1 Universidade de Vigo, Departamento de Química Orgánica, 36310 Vigo, España; Instituto de Investigación Sanitaria Galicia Sur, Hospital Álvaro Cunqueiro, 36213 Vigo, España.
  • 2 Universidade de Vigo, Departamento de Química Física, 36310 Vigo, España.
  • 3 Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica. Universidade de Santiago de Compostela, 15782 Santiago de Compostela, España.
  • 4 Universidade de Vigo, Departamento de Química Orgánica, 36310 Vigo, España; Instituto de Investigación Sanitaria Galicia Sur, Hospital Álvaro Cunqueiro, 36213 Vigo, España. Electronic address: mcteran@uvigo.es.
PMID: 38986420 DOI: 10.1016/j.bioorg.2024.107615
Abstract

A series of stilbene analogues, in which a phenyl ring was replaced by the pyridazin-3(2H)-one nucleus, was designed and synthesized to be explored as platelet aggregation inhibitors. The proposed stilbene-pyridazinone hybrids were successfully obtained from simple starting Materials and by Wittig's reaction. Most of the target compounds displayed improved in vitro activity in comparison with the standard drug, resveratrol, highlighting as the most potent the analogues 10d and 10e, with inhibition percentages of 94.15 % at 100 µM and 100 % at 50 µM, respectively. The pharmacokinetic and toxicity (ADME/T) properties of the novel hybrids were also estimated with the SwissADME and ProTox-II web servers.

Keywords

Computational approach; Molecular hybridization; Platelets; Pyridazin-3(2H)-one; Stilbene; Synthesis; in vitro Study.

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