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Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.

Authors :
Joshi, Pramod
Anderson, Corey
Binch, Hayley
Hadida, Sabine
Yoo, Sanghee
Bergeron, Danielle
Decker, Caroline
terHaar, Ernst
Moore, Jonathan
Garcia-Guzman, Miguel
Termin, Andreas
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