Calcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template

Calcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template

In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached phenyl ring, systematic SAR was carried out on both t...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2008-01, Vol.18 (2), p.755-758
Hauptverfasser: Nguyen, Diem N., Paone, Daniel V., Shaw, Anthony W., Burgey, Christopher S., Mosser, Scott D., Johnston, Victor, Salvatore, Christopher A., Leonard, Yvonne M., Miller-Stein, Cynthia M., Kane, Stefanie A., Koblan, Kenneth S., Vacca, Joseph P., Graham, Samuel L., Williams, Theresa M.
Format: Artikel
Sprache:eng
Schlagworte:
Administration, Oral
Animals
Biological and medical sciences
Biological Availability
CGRP
CGRP receptor antagonist
Half-Life
Medical sciences
Migraine
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Pyridones - administration & dosage
Pyridones - chemistry
Pyridones - pharmacokinetics
Pyridones - pharmacology
Rats
Receptors, Calcitonin Gene-Related Peptide - antagonists & inhibitors
Structure-Activity Relationship
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Beschreibung
Zusammenfassung:In our effort to find potent, orally bioavailable CGRP receptor antagonists for the treatment of migraine, a novel series based on a pyridinone template was investigated. After optimizing the privileged structure and the placement of the attached phenyl ring, systematic SAR was carried out on both the N-alkyl and C-5 aryl substituents. Several analogs with good potency and pharmacokinetic profiles were identified.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2007.11.042