Structure-activity relationship of a series of diaminoalkyl substituted benzimidazole as neuropeptide Y Y1 receptor antagonists

H Zarrinmayeh, DM Zimmerman, BE Cantrell…

Index: Zarrinmayeh, Hamideh; Zimmerman, Dennis M.; Cantrell, Buddy E.; Schober, Douglas A.; Bruns, Robert F.; Gackenheimer, Susan L.; Ornstein, Paul L.; Hipskind, Philip A.; Britton, Thomas C.; Gehlert, Donald R. Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 5 p. 647 - 652

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Citation Number: 95

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).