New ligands and pharmacological tools for the study of g protein-coupled receptors using multicomponent reactions

• Autores: Ana Mallo Abreu
• Directores de la Tesis: Eddy Sotelo Pérez (dir. tes.)
• Lectura: En la Universidade de Santiago de Compostela ( España ) en 2021
• Idioma: inglés
• Tribunal Calificador de la Tesis: Yagamare Fall Diop (presid.), María Joâo Matos (secret.), Angela Stefanachi (voc.)
• Programa de doctorado: Programa de Doctorado en Investigación y Desarrollo de Medicamentos por la Universidad de Santiago de Compostela
• Materias:
  • Química
    • Química orgánica
      • Química de carbonio
  • Ciencias médicas
    • Farmacodinámica
      • Lugar de acción activa, receptores
• Enlaces
  • Tesis en acceso abierto en: MINERVA
• Resumen

  • This PhD thesis describes the synthesis and optimization of novel families of potent and selective A2B antagonists and D2 biased partial agonists, thus contributing to the discovery of therapeutic agents for the treatment of pathologies such as cancer, schizophrenia, or Parkinson's disease. The chemical entities obtained were conceived using different design criteria and assembled using convergent, highly exploratory, and experimentally simple multicomponent reactions. The pharmacological characterization of the obtained libraries enabled the identification of A2BAR antagonists eliciting excellent potency, selectivity, and metabolic stability; as well as the identification of previously unexplored DRD2 biased partial agonists.