Download Synthesis and Characterization of Heterocyclic Derivatives as Potent and Selective Adenosine Receptors' Antagonists.

NUS Graduate School for Integrative Sciences and Engineering
Research Project Write-up
PROJECT 2
Title of Project :
SYNTHESIS AND CHARACTERIZATION OF
HETEROCYCLIC DERIVATIVES AS POTENT AND
SELECTIVE
ADENOSINE
RECEPTORS’
ANTAGONISTS
Name of Supervisor :
Giorgia Pastorin
Contact Details:
Tel: 6516 1876; email: [email protected]
Short Description
Adenosine’s receptors (A1, A2A, A2B and A3) represent promising drug targets, since
the modulation of adenosine activity, especially if very selective, might be beneficial
in certain disorders (for example cancer and inflammation (A3), asthma, type-II
diabetes, Alzheimer’s disease and cystic fibrosis (A2B)).
In particular, we are investigating some heterocyclic systems, whose basic structure
has resulted to be a potent inhibitor of these receptors, with different degrees of
affinity and selectivity. Although many details concerning these structures are now
available, a selective and potent antagonist especially towards A3 and A2B receptor
subtypes is still highly defective.
Therefore, this project is intended to obtain a certain library of compounds in order to
better understand the critical parameters that are involved in the ligand-receptor
interaction.