Diarylacetylene piperidinyl amides as novel anxiolytics

The chemistry and activity of anxiolytic diarylacetylene piperidine 9 is described. N-Phenyl-2-[1-[3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide ( 9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficac...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (11), p.3065-3067
Main Authors: Kordik, Cheryl P., Luo, Chi, Gutherman, Maryann, Vaidya, Anil H., Rosenthal, Daniel I., Crooke, Jeffrey J., McKenney, Sandra L., Plata-Salaman, Carlos R., Reitz, Allen B.
Format: Article
Language:English
Subjects:
Acetylene - chemistry
Amides - chemical synthesis
Amides - chemistry
Amides - pharmacology
Animals
Anti-Anxiety Agents - chemical synthesis
Anti-Anxiety Agents - chemistry
Anti-Anxiety Agents - pharmacology
Anxiolytics
Biological and medical sciences
CHO Cells
Cricetinae
Diarylacetylenes
Elevated plus maze
Humans
Medical sciences
Mice
Molecular Structure
Neurokinin
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Piperidines
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Sonogashira coupling
Structure-Activity Relationship
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Summary:The chemistry and activity of anxiolytic diarylacetylene piperidine 9 is described. N-Phenyl-2-[1-[3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide ( 9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficacy for the treatment of anxiety. Modest affinity was observed for the neurokinin NK-1 and 2 receptors, which are known to be involved in the regulation of mood and emotion.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.02.027