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