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Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 24:845-849
- Publication Year :
- 2014
- Publisher :
- Elsevier BV, 2014.
-
Abstract
- Calcitonin gene-related peptide (CGRP) has been implicated in acute migraine pathogenesis. In an effort to identify novel CGRP receptor antagonists for the treatment of migraine, we have discovered thiazolidinone 49, a potent (Ki=30 pM, IC50=1 nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties.
- Subjects :
- Calcitonin Gene-Related Peptide
Migraine Disorders
Clinical Biochemistry
Pharmaceutical Science
Peptide
Pharmacology
Calcitonin gene-related peptide
Biochemistry
Piperazines
Pathogenesis
Inhibitory Concentration 50
chemistry.chemical_compound
Drug Discovery
medicine
Animals
Humans
Urea
Molecular Biology
IC50
Quinazolinones
chemistry.chemical_classification
Molecular Structure
integumentary system
Organic Chemistry
Imidazoles
Antagonist
Azepines
Dipeptides
medicine.disease
Rats
Molecular Weight
nervous system
Migraine
chemistry
Calcitonin
Quinazolines
Molecular Medicine
Thiazolidinediones
Penetrant (biochemical)
Protein Binding
Receptors, Calcitonin Gene-Related Peptide
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 24
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....f1099f3ef1762ba078256019f64e4779
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.12.089