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Transcript
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.