Structure-activity relationships of a series of 1-substituted-4-methylbenzimidazole neuropeptide Y-1 receptor antagonists

The characterization of a novel series of NPY-1 receptor antagonists derived from the 4-methylbenzimidazole 4 is described. Appropriate substitution on the piperidyl nitrogen of 4 led to systematic increases in Y-1 receptor affinity, to approximately 50-fold, and to the discovery of the importance o...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1998-03, Vol.8 (5), p.473-476
Main Authors: Zimmerman, Dennis M., Cantrell, Buddy E., Smith, Edward C.R., Nixon, James A., Bruns, Robert F., Gitter, Bruce, Hipskind, Philip A., Ornstein, Paul L., Zarrinmayeh, Hamideh, Britton, Thomas C., Schober, Douglas A., Gehlert, Donald R.
Format: Article
Language:English
Subjects:
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Cell Line
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Receptors, Neuropeptide Y - antagonists & inhibitors
Recombinant Proteins - antagonists & inhibitors
Structure-Activity Relationship
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Summary:The characterization of a novel series of NPY-1 receptor antagonists derived from the 4-methylbenzimidazole 4 is described. Appropriate substitution on the piperidyl nitrogen of 4 led to systematic increases in Y-1 receptor affinity, to approximately 50-fold, and to the discovery of the importance of a second basic substituent. The characterization of a novel series of NPY-1 antagonists 3 is described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00048-1