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Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Feb2014, Vol. 24 Issue 3, p845-849. 5p. - Publication Year :
- 2014
-
Abstract
- 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 (K i =30pM, IC50 =1nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 24
- Issue :
- 3
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 94025087
- Full Text :
- https://doi.org/10.1016/j.bmcl.2013.12.089