New scaffolds in the development of mu opioid-receptor ligands

…, N Nguyen, S Bernard, M Coupal, M Gosselin…

Index: Page, Daniel; Nguyen, Natalie; Bernard, Sylvain; Coupal, Martin; Gosselin, Mylene; Lepage, Julie; Adam, Lynda; Brown, William Bioorganic and Medicinal Chemistry Letters, 2003 ,  vol. 13,  # 9  p. 1585 - 1589

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Citation Number: 11

Abstract

A new class of μ selective receptor antagonists has been developed using a combinatorial approach based on previously reported Dmt-Tic dipeptide ligands. Modified tetrahydroisoquinoline (Tiq) residues were reacted with different electrophiles in order to create novel molecules that would mimic the original dipeptide. A specific class of thioureas bearing basic pyrrolidine residues were shown to give good binding affinities. Further ...