RT Dissertation/Thesis
T1 New Ligands and Pharmacological Tools for the Study of G Protein-Coupled Receptors Using Multicomponent Reactions
A1 Mallo Abreu, Ana
K1 Multicomponent reactions
K1 Dopamine D2 receptors
K1 Adenosine A2B antagonists
K1 Hit identification in drug discovery Biased ligands
AB This PhD thesis describes the synthesis and optimization of novel families ofpotent and selective A2B antagonists and D2 biased partial agonists, thus contributing to the discovery oftherapeutic agents for the treatment of pathologies such as cancer, schizophrenia, or Parkinson's disease. Thechemical entities obtained were conceived using different design criteria and assembled using convergent, highlyexploratory, and experimentally simple multicomponent reactions. The pharmacological characterization of theobtained libraries enabled the identification of A2BAR antagonists eliciting excellent potency, selectivity, andmetabolic stability; as well as the identification of previously unexplored DRD2 biased partial agonists.
YR 2021
FD 2021
LK http://hdl.handle.net/10347/26989
UL http://hdl.handle.net/10347/26989
LA eng
DS Minerva
RD 25 abr 2026