224053-24-1Relevant articles and documents
Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: Optimization of the C-2 side chain
Britton, Thomas C.,Spinazze, Patrick G.,Hipskind, Philip A.,Zimmerman, Dennis M.,Zarrinmayeh, Hamideh,Schober, Douglas A.,Gehlert, Donald R.,Bruns, Robert F.
, p. 475 - 480 (1999)
A series of benzo[b]thiophene-derived NPY-1 receptor antagonists is described. Systematic modification of the C-2 substituent afforded a 1000- fold range in Y1 receptor affinity. Appropriate substitution at the ortho and para positions of the C-2 phenyl ether produced a synergistic effect on Y1 binding affinity, which led to the discovery of the most active ligands, 12t (K(i) = 15 nM), 12u (K(i) = 11 nM), and 12v (K(i) = 13 nM).
