Author/Authors :
Hamideh Zarrinmayeh، نويسنده , , Dennis M. Zimmerman، نويسنده , , Buddy E. Cantrell، نويسنده , , Douglas A. Schober، نويسنده , , Robert E. Bruns، نويسنده , , Susan L. Gackenheimer، نويسنده , , Paul L. Ornstein، نويسنده , , Philip A. Hipskind، نويسنده , , Thomas C. Britton، نويسنده , , Donald R. Gehlert، نويسنده ,
Abstract :
A series of benzimidazoles (4) was synthesized and evaluated in vitro as potent and selective NPY Y1 receptor antagonists. Substitution of the piperidine nitrogen of 4 with appropriate R groups resulted in compounds with more than 80-fold higher affinity at the Y1 receptor compared to the parent compound 5 (R = 11). The most potent benzimidazole in this series was 21 (Ki = 0.052 nM).
