Bioorganic and Medicinal Chemistry Letters p. 475 - 480 (1999)
Update date:2022-08-04
Topics:
Britton, Thomas C.
Spinazze, Patrick G.
Hipskind, Philip A.
Zimmerman, Dennis M.
Zarrinmayeh, Hamideh
Schober, Douglas A.
Gehlert, Donald R.
Bruns, Robert F.
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).
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