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

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

Bioorganic & Medicinal Chemistry Letters（2014）

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摘要

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=30pM, IC50=1nM), orally bioavailable, CNS-penetrant CGRP antagonist with good pharmacokinetic properties.

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关键词

Migraine,CGRP antagonists,Thiazolidinone

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