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Structure-activity relationships of a series of benzothiophene-derived NPY Y1 antagonists: optimization of the C-2
T C Britton1, P G Spinazze, P A Hipskind
1Lilly Research Laboratories, A Division of Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA.
Bioorganic & Medicinal Chemistry Letters
|March 26, 1999
Abstract:
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).